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A smoothing method for noisy experimental photoluminescence spectra distorted by narrow spectral peaks and observed in ZnS:Mn bulk crystals and nanocrystals is proposed. Use of this method makes it possible to separate slowly varying components of the photoluminescence spectrum and narrow spectral peaks caused by radiation of the He–Cd laser plasma or harmonics of N2-laser radiation that excite photoluminescence.

The study showed that the influence of alloying elements on the secondary structure formation of the steels containing from 0.19 to 0.37 wt. % carbon; 0.82-1.82 silicon; 0.63-3.03 manganese; 1.01-3.09 chromium; 0.005-0.031 nitrogen; up to 0.25 wt.% vanadium and austenite grain size is determined by their change in the content of vanadium nitride phase in austenite, its alloying and overheating above tac3, and the dispersion of ferrite-pearlite, martensitic and bainitic structures is determined by austenite grain size and thermal kinetic parameters of phase transformations. Analytical dependencies are defined that describe the experimental data with a probability of 95% and an error of 10% to 18%. An analysis results of studying the structure formation of structural steel during tempering after quenching show that the dispersion and uniformity of the distribution of carbide and nitride phases in ferrite is controlled at complete austenite homogenization by diffusion mobility and the solubility limit of carbon and nitrogen in ferrite, and secondary phase quantity in case of the secondary phase presence in austenite more than 0.04 wt. %. Equations was obtained which, with a probability of 95% and an error of 0.7 to 2.6%, describe the real process.

The applications of homology and isomerism to the structure of phase diagrams and distillation flowsheets of multicomponent mixtures were considered. Three homologous series of separation flowsheets based on combinations of distillation and splitting were studied for ternary, quaternary and five-component mixtures of water with aromatic hydrocarbons (benzene, toluene, ethylbenzene, propylbenzene). In each series, the flowsheets are ranked according to increasing energy consumption: preliminary splitting—indirect separation sequence—direct separation sequence of the initial mixture. The energy consumption depends linearly on the number of homologous components in the mixture and was shown to be predictable in flowsheets (using the system with butylbenzene as an example). A comparison of isomer flowsheets with the same number of apparatuses but with different sequences of product separation showed that the indirect separation sequence is energetically preferable provided that the water and benzene product flows are separated in the form of equilibrium liquid phases from a decanter.

The infiltration of aluminum melts into porous metal skeletons produced by powder metallurgy methods, including 3D printing, under a pressure gradient was studied. The densification of compacts made of iron powder with various blowing additions was examined. The minimum pressures at which 35–40% porosity was reached were found to be 150–200 MPa. The use of metal iron shavings allowed a porous skeleton to be formed at a lower pressure (100 MPa). The minimum pore size (400 μm) ensuring complete filling of the porous skeleton with an aluminum melt heated to 760–780°C under a pressure gradient was established. The potential production of iron–aluminum composites without the formation of chemical compounds was shown. A thin discrete layer 5–10 μm thick was observed at the interface between iron and aluminum, where the iron skeleton became saturated with aluminum. This layer provides better adhesion between the iron skeleton and the aluminum melt. The absence of chemical compounds in the Fe–Al system in impregnation conditions is explained by the process kinetics: the components cannot react with each other within several seconds. The effect exerted by the type of porous skeletal structure on the compressive strain of the iron–aluminum composites was established. The greatest compression strength (~400 MPa) was shown by the samples produced from 3D skeletons. The stress–strain curves for the samples with 3D skeletons show two bends: one is in the range 60–70 MPa (beginning of plastic deformation) where strain hardening occurs and strain increases to 20–22% and the other begins at 230–240 MPa and determines the bulk deformation of the samples. The highest yield stress was observed for the samples with shavings-based skeletons (115.2 MPa), which is associated with a high contact surface area of the shaving particles that are randomly intertwined. Accordingly, the lowest characteristics were shown by the samples with skeletons consisting of powder particles with the minimum contact area.

Background Intra-articular injections of corticosteroids (CCS), hyaluronic acid (HA), and platelet-rich plasma (PRP) have often been used for temporomandibular joint osteoarthritis (TMJ OA). However, there is no guideline for the choice of pharmacological injections. The aim of this network meta-analysis (NMA) is to compare the efficacy of different intra-articular injectable treatments on TMJ OA. Methods Studies were identified from PubMed, Embase and Cochrane Central with date up to December 2020. Randomized Controlled Trials (RCTs) included were the studies of patients with TMJ OA who had intra-articular treatment with CCS, HA, PRP, placebo and follow-up assessing TMJ function in target outcome variables. The primary outcome was temporomandibular joint pain (VAS). The secondary outcomes were maximal mouth opening (mm), and lateral movement to the affected side (mm). Results Nine RCTs involving 316 patients were included. For primary pain outcome, no significance was detected when CCS, HA and PRP were compared with placebo by both short- (3-6 months) and long-term (>12 months) follow-up. In addition, these injectables did not significantly outperform placebo by evaluating secondary functional outcomes (maximal mouth opening and lateral movement) with the same follow-up. Subgroup analyses showed that the effect of CCS on subgroups with more than 70% women was statistically less effective compared with placebo. Conclusion Evidence suggested that intra-articular pharmacological injections of CCS, HA, and PRP had no effect on improving TMJ pain and functional outcomes compared with placebo injection. Trial registration This study is registered with PROSPERO, number CRD42021270914.

The results of comparative studies of feline viral rhinotracheitis virus for its culture properties in primary and continuous cell cultures of feline origin (FK, FK (subculture), CrFK, FS, CC-81, FC/Tg) are presented. It was found that viral rhinotracheitis virus replication, irrespective of the route of infection and the culture technique, was consistent and practically equal in susceptible cell cultures. The most pronounced cytopathic effect (more than 75% monolayer degeneration) was observed in all types of cell cultures in 48–72 hours of cultivation. However, the accumulation of feline viral rhinotracheitis virus Grand strain was highest when preliminary adsorption occurred within the specified period of time, monolayer cell cultures were infected with the virus at a dose of 5.5 lg TCID50/ml and roller bottle cultivated, and the рН of the medium was maintained at 7.0–7.4. Single freezing of the virus at a temperature of minus 60 degrees Celsius upon the completion of the cultivation cycle (during 60–72 hours) and its thawing were found to significantly increase the virus titre by 0.5 lg TCID50/ml.

Physical and chemical testing of sulfate product, obtained as a result of high-temperature treatment of ore from the Kundybai field with sulfuric acid mixture at 500°C revealed the presence of cerium oxide corresponding to natural cerianite (CeO2). A mechanism of its formation is proposed, which includes a stage of cerium sulfate (Ce(SO4)2) formation followed by its dissociation to CeO2. The presence of this compound in the sulfate product allowed establishing the temperature required to further conduct the sulfation process and prevent cerianite formation.

The successful use of drugs, derivatives of 1,2,4-triazole, creates the conditionsfor the production and investigation of properties of new derivatives of this heterocyclic system. The aim of this work was synthesis and study of physical and chemical properties of new derivatives of 1,2,4-triazole-3-thiol containing synthon of pyrrole. The object of the study was a 4-phenyl-5-(pyrrol-2-yl)-1,2,4-triazole-3-ylthio-R-carbothioamides. To achieve this goal it was necessary to solve following tasks: to conduct the selection of the optimum base structure to determine the most efficient way of chemical modification of the precursor of targeted synthesis, to carry out selection of necessary methods of synthesis, to investigate the physico-chemical properties and to set the structure of the obtained compounds. The synthesis of target products of the reaction was carried out using as starting material pyrrole, which with using the form non-catalytic form of reaction of the Fridel-Crafts was transformed into 2,2,2-trichloro-1-(pyrrol-2-yl), ethanol. The resulting material in the result of reaction of hydrazinolysis was converted into the pyrrol-2-carbohydrazide. The obtained intermediate product was used in the reaction of nucleophilic joining of phenylisothiocyanate with subsequent intramolecular alkaline heterocyclization. Synthesized thiol was used in the reaction of alkylation. The structure of the obtained substances are confirmed by using elemental analysis, 1H-NMR-spectroscopy, and their individuality – chromatographic methods of analysis. The resulting substances are an interesting object for further studies, especially biological activity.

Derivatives of 1,2,4-triazole are inherent in various types of biological activity. They can be used as pesticide and medicinal drugs (anticonvulsants, analgetics, antitumor and antibacterial). In this regard the search of new methods of synthesis and investigation of biological activity of 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio)acetate acids and their salts is relevant nowadays. With the aim of finding the new biologically active compounds 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio)acetate acids and their salts are synthesized, where R is methyl, ethyl, phenyl. The interaction of 4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thions with monochloracetate acid in the medium of i-propyl alcohol in the presence of an equivalent amount of alkali the corresponding 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4 triazole-3-ylthio)acetate acids are obtained on the basis of which the corresponding salts of morpholine, dimethylamine, monoethanolamine, pteridine, ZnSO4 , CuSO4, NaOH and KOH are obtained and the structure of the received compounds was confirmed on the basis of the data of elemental, IR-, 1H-NMR-spectroscopy. The synthesis of 2-(4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio) acetate acids and their salts was conducted. With the help of modern physico-chemical methods: elemental analysis, IR, 1H-NMR-spectroscopy the structure of synthesized compounds, and their individuality by HPLC-MS is proved. In the IR spectrum of the compound 2-(4-phenyl-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-ylthio)acetate acid Ic available band fluctuations groups characteristic for the nucleus of 1,2,4-triazole: NH– in the range of 3 400–3 100 cm-1,–C=N– – 1 690–1 620 cm-1. Also present band fluctuations groups –C–S– at 691 cm-1. Available band fluctuations characteristic of the group –CH2 within 1496.59 cm-1 and group –COO-H– – 1722.70 cm-1. This suggests the possibility to further study the biological action of the synthesized compounds.

Purposeful synthesis of derivatives of 1,2,4-triazole is one of the most important branches of modern pharmaceutical science Modern pharmaceutical market of domestic medicines requires constant updates of existing range. It makes possible the synthesis of new compounds with a predicted biological activity. The main advantage of derivatives of 1,2,4-triazole is high efficiency and low toxic. That is promising factor for creation of new chemical compounds. Analysis of literary data of past few years has showed that there is not enough information about synthesis, physical, chemical and biological properties of derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol in the literature. So synthesis and further research of derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol is topical. The research took place at the Department of toxicological and inorganic Chemistry of Zaporizhzhia State Medical University (the head of the department – professor O. I. Panasenko). During the work the research were the physicochemical properties of newly synthesized of compounds in accordance with the methods described in the State Pharmacopoeia of Ukraine. As starting substance was used 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol obtained by cyclization of of potassium 2-atsetilgidrazinkarboditioata in the medium hydrazine hydrate. It is planned to research of the compounds obtained in the antimicrobial, act-protective, antioxidative and hypolipidemic activity. 9 new compounds of ylidene derivatives of 4-amino-5-methyl-4H-1,2,4-triazole-3-thiol were synthesized in a research. The structure of the new synthesized of substances was confirmed by with by means of modern of instrumental methods analysis (1H-PMR-spectroscopy, chromato-mass-spectrometry, elemental analysis). The obtained data is possible to use in purposeful synthesis for the further research of biologically active compounds.

Phosphorus slag is the most heavy-tonnage waste of yellow phosphorus production, which is stored in the dump fields for many years causing ecological problems in the regions. One of the relevant and priority directions is rare-earth metals (REMs) production, presence of which in the phosphorus slags allows considering the latter as an acceptable raw material source. Phosphorus slags contain about 30–40 wt% of silicon dioxide, therefore they can serve as a source of production of precipitated silicon dioxide highly required in different industries. The purpose of this work is studying the conditions for REMs recovery from phosphorus slag and further processing of silicon-containing cake to improve a quality of the obtained products.The work shows results of researches on the phosphorus slags’ chemical and phase compositions identification, processes of leaching of phosphorus slag and the obtained silicon-containing cake by nitric acid. Instrumental and chemical methods of phosphorus slag content analysis give following data. It consists of 90–92 % of pseudowollastonite α-CaSiO3, and also there are gyrolite Ca4(H2O)4[Si6O15](OH)2, small amounts of serpentine Mg6[Si4O10](OH)8, hydrated calcium aluminosilicate impurities CaO∙2Al2O3∙2SiO2∙H2O, quartz α-SiO2, calcite CaCO3, hematite Fe2O3, iron phosphate FePO4 and metallic iron with manganese impurity. As a result of kinetic studies of leaching process of phosphorus slag, the apparent activation energy for ΣREMs, calcium, aluminum and iron was determined which amounted to 4.31, 8.53, 7.43 and 12.31 kJ/mol, respectively. This, in combination with value of the Pilling-Bedward Criterion CP-B = 1.1 for orthosilicate acid H4SiO4, indicates that the process is characterized by an intradiffusion region. With a decrease in temperature of nitric acid treatment from 90 to 70 °C, purification degree of precipitated silicon dioxide from iron and aluminium impurities increases. Results of the experimental data will serve as a basis for development of the technology for complex processing of production waste of phosphorus industry and for improving quality of obtained products as REMs concentrate and precipitated silicon dioxide.

A possibility of the two-photon excitation of an isomeric state in a nucleus of thorium-229 has been discussed. The fluorescence intensity of the excitation is demonstrated to be identical for the irradiation of nuclei with either monochromatic light or polychromatic radiation consisting of a sequence of short light pulses of the same intensity. The two-photon excitation of Th^{3+} ion in an electromagnetic trap with a focused laser beam with a wavelength of about 320 nm and power of 100 mW can lead to the absorption saturation, at which the fluorescence emission with the frequency of the transition in a nucleus is maximal. In crystals doped with Th^{4+} to a concentration of about 10^{18} cm^{-3} and irradiated with a laser radiation 10 W in power, the emission of several photons per second with a wavelength of about 160 nm becomes possible., Comment: 13 pages, 1 figure; http://www.ujp.bitp.kiev.ua

Today, an increase of natural and technogenic situations leads to the disorders of the central nervous system, functional-metabolic processes, vascular diseases, in particular, acute cerebral blood flow disorders. In addition, the changes occurring on the molecular and cellular levels are in the basis of the functional violations of individual systems and the organism as a whole. Hypoxia not only complicates the disease course, but in most cases, determines its outcome. The important role in the fight against hypoxia belongs to antioxidants, which improve the circulating oxygen utilization by the body, reduce its need for the organs and tissues, which is not only expedient but necessary for the treatment of many acute and chronic pathological processes. So, the frequency of the hypoxic states and a wide range of factors causing them determine the relevance of new ways and methods finding to overcome the oxygen deficiency. The aim of this work is the purposeful search of some 5-[((5-(adamantane-1-yl)-4-R-4H-1,2,4-triazole-3-yl)thio)methyl]-N-R1-1,3,4-thiadiazole-2-amines and 5-[((5-(adamantane-1-yl)-4-R-4H-1,2,4-triazole-3-yl)thio)methyl]-4-R1-4H-1,2,4-triazole-3-thiols, the study of their physical and chemical properties and pharmacological screening of the antihypoxic activity of the obtained compounds. Materials and methods. The study of physical and chemical properties was conducted on certified and licensed modern equipment. Antihypoxic activity was studied during the modeling process of hypoxia with hypercapnia. Mexidol was used as a comparison drug in studies at a dose of 100 mg/kg. Results. As the result of the study, it was found that the synthesized compounds and the comparison drug influenced on rats’ life span differently. Compounds, the antihypoxic activity of which exceeded control have been discovered, and others’ were at the level of Mexidol. A number of compounds showed a somewhat less activity in comparison with control, and two compounds, among the investigated ones were weaker then comparison drug action, but they did not reduce the life expectancy of the investigated groups in comparison with control. The effect of the remaining compounds on the lifetime of the investigated group was at the level of control group that received the physiological solution. Conclusions. A series of new compounds of derivatives among 5-[((5-(adamantane-1-yl)-4-R-4H-1,2,4-triazol-3-yl)thio)methyl]-N-R1-1,3,4-thiadiazole-2-amines and 5-(5-(adamantane-1-yl)-4-R-4H-1,2,4-triazole-3-yl)thio)methyl)-4-R1-4H-1,2,4-triazole-3-thiols have been synthesized, the structure of which has been confirmed with the help of modern physical and chemical methods of analysis. The most active compounds among the studied ones were 3a and 2a, their antihypoxic activity exceeds control on 37.86 % and 36.30 % and Mexidol is on 7.35 % and 5.79 % respectively.

Актуальность поиска новых биологически активных соединений среди производных 1,2,4-триазола не вызывает никаких сомнений. Перспективность этого направления подтверждена многими публикациями как отечественных, так и иностранных ученых. Известно, что различные производные 1,2,4-триазола малотоксичны или практически нетоксичны, обладая при этом широким спектром биологического действия. Одним из основных приоритетов внедрения новых веществ является их незначительная токсичность. Поэтому целенаправленный синтез малотоксичных соединений и ориентированное изучение острой токсичности являются первоочередными задачами на пути фармакологических исследований.Цель работы – изучение острой токсичности впервые синтезированных S-производных 4-R-5-(тиофен-2-илметил)-4Н-1,2,4-триазола.Материалы и методы. Для изучения острой токсичности выбрали табличный экспресс-метод по В. Б. Прозоровскому, в основе которого лежит предложение использовать изучаемые вещества в дозах, размещенных в логарифмической шкале с интервалом 0,1, а все возможные достоверные результаты LD50 и их погрешности рассчитаны предварительно по программе пробит-анализа.Результаты. В результате проведенных исследований установлено, что острая токсичность синтезированных соединений находится в пределах 193–770 мг/кг. Согласно классификации К. К. Сидорова, они относятся к малотоксичным или практически нетоксичным соединениям. Наиболее токсичным соединением среди тиолов является 4-метил-5-(тиофен-2-илметил)-4H-1,2,4-триазол-3-тиол – 304 ± 65 мг/кг. Острая токсичность N'-R1-иден-2-((4-метил-5-(тиофен-2-илметил)-4H-1,2,4-триазол-3-илтио)ацетогидразидов находится в пределах 193–770 мг/кг.Выводы. Изучена острая токсичность S-производных 4-R-5-(тиофен-2-илметил)-4Н-1,2,4-триазола, которая находится в пределах 193–770 мг/кг. Выявлены некоторые закономерности «структура – острая токсичность»., The urgency of the search for new biologically active compounds among the 1,2,4-triasole derivatives is beyond doubt. The promise of this direction has been confirmed by many publications by both domestic and foreign scientists. It is known that various derivatives of 1,2,4-triazole are low-toxic or practically non-toxic compounds, while possessing a wide range of biological effects. As we know, one of the main priorities of the introduction of new substances is a minor toxicity. Therefore, purposeful synthesis of low-toxic compounds and focused study of acute toxicity are the priority tasks of pharmacological research.The aim of the work was to study the acute toxicity of the first synthesized S-derivatives of 4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazoles.Materials and methods. An express method of V. B. Prozorovsky was selected for the study of acute toxicity. The basis of this method is the use of test substances in doses located on a logarithmic scale with an interval of 0.1, and all possible reliable LD50 results and their errors are calculated by pre-program of the probit analysis.Results. As a result of the studies, it was found that the acute toxicity of the synthesized compounds is within the limits of 193–770 mg/kg. According to K. K. Sidorov classification they are low-toxic or practically non-toxic compounds. The most toxic compound among thioles is 4-methyl-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol – 304 ± 65 mg/kg. The acute toxicity of N'-R1-iden-2-((4-methyl-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-ylthio)acetohydrazides are within the range of 193–770 mg/kg.Conclusions. The acute toxicity of 4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazoles S-derivatives is found to be within the range of 193–770 mg/kg. Some patterns of "structure-acute toxicity" are revealed., Актуальність пошуку нових біологічно-активних сполук серед похідних 1,2,4-тріазолу не викликає жодних сумнівів. Перспективність цього напряму підтверджена багатьма публікаціями як вітчизняних, так і закордонних вчених. Відомо, що різні похідні 1,2,4-тріазолу є малотоксичними або практично не-токсичними сполуками, володіючи при цьому широким спектром біологічної дії. Одним з основних пріоритетів впровадження нових речовин є незначна токсичність. Отже, цілеспрямований синтез малотоксичних сполук та орієнтоване вивчення гострої токсичності – першочергові завдання на шляху фармакологічних досліджень.Мета роботи – вивчення гострої токсичності вперше синтезованих S-похідних 4-R-5-(тіофен-2-ілметил)-4Н-1,2,4-тріазолів.Матеріали та методи. Для вивчення гострої токсичності обрали табличний експрес-метод за В. Б. Прозоровським, в основі якого – пропозиція використовувати досліджувані речовини в дозах, котрі розміщені в логарифмічній шкалі з інтервалом 0,1, а всі можливі вірогідні результати LD50 та їхні похибки розраховані попередньо по програмі пробіт-аналізу.Результати. Встановили, що гостра токсичність синтезованих сполук перебуває в межах 193–770 мг/кг. Згідно з класифікацією К. К. Сидорова, вони належать до малотоксичних, або практично нетоксичних сполук. Найтоксичнішою сполукою серед тіолів є 4-метил-5-(тіофен-2-ілметил)-4H-1,2,4-тріазол-3-тіол (304 ± 65 мг/кг). Гостра токсичність N'-R1-іден-2-((4-метил-5-(тіофен-2-ілметил)-4H-1,2,4-тріазол-3-ілтіо)ацетогідразидів перебуває в межах 193–770 мг/кг.Висновки. Вивчено гостру токсичність S-похідних 4-R-5-(тіофен-2-ілметил)-4Н-1,2,4-тріазолів, що перебуває в межах 193–770 мг/кг. Виявлено деякі закономірності «структура – гостра токсичність».

In recent years we see significant increase of natural and technogenic situations that lead to disorders of functional and metabolic processes of central nervous system and cardiovascular diseases, including acute cerebrovascular accident. The leading factor in vascular brain pathology is hypoxia. Currently all body states, in which we see any reason decrease of oxygen delivery to tissues is considered as hypoxia. Paying into account the fact that available pharmacotherapeutic agents for the oxygen deficiency treatment tend to have limited efficacy, narrow range of active doses and often cause undesirable side effects, the special attention is paid to drugs that have an antihypoxic action and exclude the above mentioned effects. Aim. To study antihypoxic actions for the first time synthesized derivatives of 1,2,4-triazoles and to find the "structure - action" dependence. Materials and methods . Antihypoxic activity of 1,2,4-triazoles derivatives was studied at modeling hypoxia with hypercapnia. Rats were placed in same volume (1330 ml) sealed up jars, then overturned them down and put in a cell with water to prevent the flow of air. As a comparison drug in the study we used mexidol 100 mg / kg. Results . The study has identified three compounds that extend the comparison drug mexidol and prolong the life expectancy of 59.94 %, 47.79% and 53.31% (compounds 1, 2, 5, respectively). While mexidol was 42.54%. After analyzing the data and chemical structure of the synthesized compounds we have established some relative patterns between chemical structure and antihypoxic actions of 1,2,4-triazoles derivatives. Conclusions . As the result of the study, we have discovered the compound that exceeds the referent drug mexidol on 17.4%. In the study of the acute toxicity of 1,2,4-triazoles derivatives it was found that all compounds belong to IV Class of toxicity (LD 50 = 331-770 mg / kg). The presence of two halogen atoms in the molecules of benzylidenhydrazides of 4-R-5-(thiophene-2-ylmethyl)-1,2,4-triazol-3-il) thioacetic acid shows expressive antihypoxic action.

The phase composition and unit cell parameters were determined for composites based on polylactide and hydroxyapatite with the polylactide/hydroxyapatite weight ratios of 90/10, 80/20, 70/30, and 60/40. As the polylactide content of the composites is increased, they become less hydrophilic, and the surface energy σS-G increases from 29.13 to 74.35 mJ m–2. The sample with the component weight ratio of 70/30 is characterized by the maximal roughness, and the Ca2+ and Mg2+ ions from simulated body fluid are actively adsorbed onto its surface, as proved by SEM examination of the composites.

In the contemporary world of high technologies lithium (Li) is a key component. Kazakhstan has the required potential for its production. The most attractive raw materials for lithium extraction are natural and saline lake brines. Investigation and search of new technological solutions with the purpose of inclusion thereof in the sphere of lithium-containing hydromineral raw material processing is an important and relevant scientific and technical task. This article provides analysis of the literature data on lithium sorption by organic resins and inorganic sorbents. Generally, cation exchange resins, both in protonated and sodium forms, are mostly used for lithium sorption. They include widespread cationite KU-2-8 or its equivalents. In the investigations on lithium sorption extraction from lithium-containing solutions from amongst of inorganic sorbents mainly manganese, titanium and aluminum based compounds are used. For the static lithium extraction from natural brines we performed sorption using ion-exchange resins: CU-2-8, Purolite C100, Purolite C160S, Purolite S940, Amberlite IR 120, CYBBER CRX 210, and CYBBER CRX 300. It was demonstrated that almost no lithium is sorbed on ionites. Insignificant amount of lithium was extracted on sulphocationite CU-2-8 and made up 0.49%. Investigations were made on natural brines processing using inorganic sorbents (in the form of commercial reagents): aluminum hydroxide, titanium and manganese oxides, and activated carbon. Besides, such inorganic sorbents as aluminum hydroxide, hydrated titanium and manganese oxides were synthesized. It was established that the highest rates were achieved when aluminum hydroxide was used as sorbent, at that lithium extraction made up 21.87%, and on synthesized sorbent - hydrated manganese oxide, where Li extraction reached 20.11%. For lithium extraction from brines inorganic sorbents were chosen as the sorption method using aluminum and/or manganese compounds as sorbents.

Significance. Nowadays non-steroidal anti-inflammatory drugs have found a wide application in treatment of medical conditions. Despite the clinical effectiveness of non-steroidal anti-inflammatory drugs, their administration is followed by a set of side effects. With aim to reveal the substances with a potency of altering pain threshold in animals, the action of 4-amino-5-methyl-4 H -1,2,4-triazol-3-thiones on the nociceptive system in conditions of thermal irritation of rats’ extremities was studied. Aim. Study of the analgesic activity of 4-amino-5-methyl-4 H -1,2,4-triazol-3-thiones. Materials and methods. Analgesic activity of the synthesized compounds was evaluated in terms of the set of experiments conducted on white rats of 180-240 g weight. The primary pain threshold after the administration of the substances was assessed using a “hot plate” test, involving a metal plate heated at 55 o C as an irritator. The time of the corresponding response (paw licking, jumping out, squeaking) was measured in seconds. Analgesic activity was assessed by observations of the alterations of pain threshold of the group of studied animals to whom the substances of research were administrated, comparing results with the control group and expressing them in percent. Results. According to the results, it was concluded that the compound of 4-(3,4-dimethoxebenzylidenamino)-5-methyl-4 H -1,2,4-triazol-3-thione was the most potent, which reduced the sensitivity to thermal irritation of extremities in the group of animals by 127.78%; that said, its activity is higher than that for the reference drug Analgin, which was also evaluated in a “hot plate” test. It was established that substance (IV) was slightly more active than the reference drug Analgin, demonstrating 121.11% of analgesic activity. Processing of the experimental data revealed some dependencies between the chemical structure and pharmacological activity of the substances of research. Conclusion. The obtained results demonstrate that analgesic activity is existent among the set of 1,2,4-triazole derivatives, which mandates a deeper research of the effectiveness and safety of the most active compounds among the studied compounds.

The article presents highly reproducible and inexpensive protocol for simultaneous demonstration of glutamate decarboxylase (GAD67), the key enzyme of gamma-aminobutyric acid (GABA) synthesis and synaptophysin (SYP), a marker protein of synaptic vesicles using confocal laser microscopy. In the cerebellar cortex, GAD labels Purkinje cells and pinceaux in their basal parts and is unevenly distributed in the neuropil of molecular and granular layers. SYP clearly marks the contours of large dendrites of Purkinje cells in molecular layer, while in the granular layers it labels parts of cerebellar glomeruli--the terminals of the mossy fibers. GAD-immunopositive structures (GABA-ergic axons of stellate cells--Golgi cells) are often located at periphery of the glomeruli. In the peripheral zone of the glomeruli, colocalization of GAD- and SYP-immunopositive structures was observed, suggesting the presence of GABA-ergic synapses in this zone.

The amount of antibiotics has increased over the past decade. This also resulted in increase of microorganisms’ resistance to this class of drugs. Therefore, the synthesis of new compounds that have exhibited antimicrobial and antifungal activity and low level of side effects is an important issue of modern pharmacy. The 1,2,4-triazole system is very promising in this aspect. The aim was to study the antimicrobial and antifungal activity of 4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol and 3-(alkylthio)-4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole. Methods and results. In the study "serial dilutions" method has been used. The criteria for the activity of given compound was the minimum inhibitory concentration (MIC) which is the lowest concentration of drug that inhibits the growth of the test culture and the minimum bactericidal concentration (MBC) which is the lowest concentration of drug that causes bactericidal effect. Test compounds are derivatives of 4-R-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol and 3-(alkyl-thio)-4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole which exhibit antifungal and antimicrobial activity. Conclusion. The most active of the studied 1,2,4-triazole derivatives is 4 (4-methyl-3-(octylthio)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole), which manifests as antifungal and antimicrobial activity. Some regularity between structure and action has been investigated.

З метою дослідження карбонільних похідних 7-((3-тіо-4-R-4H-1,2,4-тріазол-5-іл)метил)теофіліну виконали синтез вихідної речовини та її взаємодію з рядом α-галогенкетонів. Досліджені фізико-хімічні властивості одержаних сполук і підтверджена їхня будова за допомогою елементного аналізу, ІЧ-спектрометрії, 1Н ЯМР-спектрометрії, УФ-спектрофотометрії та хромато-мас-спектрометрії. Здійснили попереднє комп’ютерне дослідження гострої токсичності та біологічної активності. Встановили, що отримані сполуки можуть проявляти діуретичну й аналептичну активності, а фрагмент 1,2,4-тріазолу теоретично може підсилювати цю активність. Попереднє прогнозування гострої токсичності показало: сполуки належать до малотоксичних., Aim. To analyze the carbonyl derivatives of 7-((3-thio-4-R-4H-1,2,4-triazole-5-yl)methyl)theophylline their mother substance was synthesized and its interaction with α-haloketones series was carried out.Methods and results. The physical-chemical properties of the obtained compounds have been studied and their structures have been confirmed by elemental analysis, infrared spectrometry, 1H NMR spectrometry, UV spectrophotometry and gas chromatography mass spectrometry. Preliminary computer study of acute toxicity and biological activity has been also carried out. It has been determined that the obtained compounds may exhibit diuretic and analeptic activity and 1,2,4-triazole fragment can theoretically increase it.Conclusion. Preliminary prediction of acute toxicity has showed that the compounds are low-toxic., С целью исследования карбонильных производных 7-((3-тио-4-R-4H-1,2,4-триазол-5-ил)метил)теофиллина, проведен синтез исходного вещества и его взаимодействие с рядом α-галогенкетонов. Исследованы физико-химические свойства полученных соединений и подтверждено их строение с помощью элементного анализа, ИК-спектрометрии, 1Н ЯМР-спектрометрии, УФ-спектрофотометрии и хромато-масс-спектрометрии. Проведенное предварительное компьютерное исследование острой токсичности и биологической активности. Установлено, что полученные соединения могут проявлять диуретические и аналептические активности, а фрагмент 1,2,4-триазола теоретически может усиливать эту активность. Предварительное прогнозирование острой токсичности показало, что соединения относятся к малотоксичным.

Composites based on lactic acid oligomers, calcium hydrophosphate and hydroxyapatite synthesized under the action of microwave radiation were obtained in situ. The appearance of a new band associated with stretching vibrations of >C=O in spectra of the chloroform-insoluble fraction is indicative of the chemical interaction between lactic acid and hydroxyapatite. To determine whether a calcium phosphate layer can be formed on the surface of composite samples, biomimetic studies in a physiological SBF solution were carried out during 28 days at 37°C. It was found that all samples containing calcium phosphates promote active formation of a new calcium phosphate layer, whereas lactic acid oligomer in samples containing no inorganic component undergoes destruction in the SBF solution as a result of hydrolysis. The estimate of the resorption rate demonstrated that the solubility of calcium phosphates contained in the composites at 20°C in the physiological solution is 3–7 times that of pure hydroxyapatite.

Aim. A number of new 3,5-R-4-(3-(5-nitrofuran-2-yl)allylidenami-no)-1-R 1 -4 H -1,2,4-triazole halides have been synthesized, the structure of synthesized compounds has been proved by modern physical-chemical methods. Methods and results. Experimental substantiation of the antimicrobial activity of newly synthesized derivatives of 3,5-R-4-(3-(5-nitrofuran-2-yl)allylidenamino)-1-R 1 -4 H -1,2,4-triazole halides using disco-diffusion method on Mueller Hinton medium has been performed. Conclusion. Analysis of the results of microbiological research allowed to determine the substituent’s influence on the antimicrobial activity of 3,5-R-4-(3-(5-nitrofurans-2-yl)allylidenamino)-1-R 1 -4H-1,2,4-triazolo halides derivatives. The results indicate the prospects for further study.

The effect of mechanical vibrations on the structure formation and mechanical properties of compacts during electron beam sintering is investigated. Using optical microscopy, continuous indentation, and X-ray diffraction, it was established that imposing mechanical vibrations decreases the average titanium grain size by a factor of 1.5–2 and induces residual compressive stresses in the sintered titanium compact. Due to the stresses, greater density, and smaller grains, the ductility and compressive strength of the compacts sintered under mechanical vibrations are higher than those of the compacts sintered in conventional way.

История создания новых биологически активных субстанций берет начало еще со времен Древнего Египта. С каждым годом ученые совершенствовали методики синтеза БАВ, находили новые субстанции и вели поиск перспективных соединений для создания лекарств. В 21 веке на планете в день синтезируется более миллиона новых соединений и только некоторые из них могут в перспективе стать лекарством. Рассматривая синтетические возможности отечественной науки, следует отметить производные 1,2,4-триазола как потенциальные субстанции с различными видами биологической активности, на основе которых могут быть созданы оригинальные лекарственные средства.Цель работы – синтез и подтверждение структуры солей 2-((4-(R-амино)-5-(тиофен-2-илметил)-4H-1,2,4-триазол-3-ил)тио)ацетатных кислот.Материалы и методы. В качестве исходных веществ нами были использованы 2-((4-(R-амино)-5-(тиофен-2-илметил)-4H-1,2,4-триазол-3-ил)тио)ацетатные кислоты, синтезированные по ранее описанной методике.Строение синтезированных соединений подтверждено комплексным использованием современных физико-химических методов анализа: элементного анализа, 1H-ЯМР-спектроскопии, ВЭЖХ-МС.Результаты. Соли 2-((4-(R-амино)-5-(тиофен-2-илметил)-4H-1,2,4-триазол-3-ил)тио)ацетатной кислоты получены взаимодействием соответствующих кислот с органическими (морфолин, метиламин, моноэтаноламин), неорганическими основаниями (водный раствор аммиака, натрий гидроксид) и солями (цинк сульфат, железа (III) хлорид, магний сульфат, меди сульфат) в спиртовой или водной средах.Выводы. Синтезирован ряд новых солей 2-((4-(R-амино)-5-(тиофен-2-илметил)-4H-1,2,4-триазол-3-ил)тио)ацетатных кислот, строение которых установлено с помощью современных физико-химических методов анализа., Thanks to the rapid development of science, humanity has achieved remarkable success in various fields. This also applies to the synthesis of biological compounds. Over the centuries, scientists have invented many methods and drugs that are being actively used to date. Derivatives of 1,2,4-triazole can be the foundation for the manufacture of new native drugs that will compete with foreign ones.The aim of work was synthesis and confirmation the structure of 2-((4-(R-amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetate acids salts.Materials and methods. As starting substances we used 2-((4-(R-amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetic acids, which were synthesized by previously described methods.The structure of synthesized compounds was confirmed by the complex use of modern physical-chemical methods of analysis: elemental analysis, 1H-NMR spectroscopy, HPLC-MS.Results. Salts of 2-((4-(R-amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetic acids were synthesized by the interaction of the appropriate acids with organic (morpholin, methanamin, 2-hydroxyethanamin), inorganic basics (aqueous ammonia solution, sodium hydroxide) and salts (zinc sulfate, ferrum (III) chloride, magnesium sulfate, copper (II) sulfate) in alcoholic or aqueous media.Conclusions. A series of novel 2-((4-(R-amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazol-3-yl)thio)acetic acids salts were synthesized. The structure of synthesized compounds is established using modern physical-chemical methods of analysis., Історія створення нових біологічно-активних субстанцій бере початок ще з часів Стародавнього Єгипту. З кожним роком учені вдосконалювали методики синтезу БАР, створювали нові субстанції та провадили пошук перспективних сполук для створення ліків. У 21 столітті на планеті в день синтезується понад мільйон нових сполук, але тільки деякі з них можуть у перспективі стати ліками. Розглядаючи синтетичні можливості вітчизняної науки, варто відзначити похідні 1,2,4-тріазолу як потенційні субстанції з різними видами біологічної активності, на основі яких можуть бути створені оригінальні лікарські засоби.Мета роботи – синтез і підтвердження будови солей 2-((4-(R-аміно)-5-(тіофен-2-ілметил)-4H-1,2,4-тріазол-3-іл)тіо)ацетатних кислот.Матеріали та методи. Як вихідні речовини нами використані 2-((4-(R-аміно)-5-(тіофен-2-ілметил)-4H-1,2,4-тріазол-3-іл)тіо)ацетатні кислоти, що синтезовані за раніше описаною методикою.Будову синтезованих сполук підтверджено комплексним використанням сучасних фізико-хімічних методів аналізу: елементного аналізу, 1Н-ЯМР-спектроскопії, ВЕРХ-МС.Результати. Солі 2-((4-(R-аміно)-5-(тіофен-2-ілметил)-4H-1,2,4-тріазол-3-іл)тіо)ацетатної кислоти отримані взаємодією відповідних кислот з органічними (морфолін, метиламін, моноетаноламін), неорганічними основами (водний розчин амоніаку, натрій гідроксид) і солями (цинк сульфат, ферум (III) хлорид, магній сульфат, купрум сульфат) у спиртовому або водному середовищах.Висновки. Синтезовано ряд нових солей 2-((4-(R-аміно)-5-(тіофен-2-ілметил)-4H-1,2,4-тріазол-3-іл)тіо)ацетатних кислот, будова яких встановлена за допомогою сучасних фізико-хімічних методів аналізу.

Aim . Analysis of the scientific literature over the past decade has shown that large synthetic possibilities towards creating new and effective drug substances have heterocyclic compounds, in particular the derivatives of 1,2,4-triazole. 1,2,4-Triazole is a structural fragment of many synthetic drugs. The special interest cause ylidene hydrazides of 2-(5-R-1,2,4-triazole-3-ylthio)acetic acids as potential biologically active compounds, among which highly effective medicines can be found. With the aim of finding new biologically active compounds the derivatives of 2-((4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-yl)thio)aceticohydrazides have been synthesized, their physical-chemical properties have been studied with the use of modern methods, namely elemental analysis, IR, 1 H-NMR spectroscopy, and their individuality by HPLC-MS. Materials and methods . N'-R 1 -еden-2-((4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-yl)thio)aceticohydrazides were received by adding aromatic (2-BrC 6 H 4 , 2,3-(OCH 3 ) 2 C 6 H 3 , 3,5-(OCH 3 ) 2 C 6 H 3 , 4-N(CH 3 ) 2 C 6 H 4 , 3,4-F 2 C 6 H 3 , 2-NO 2 C 6 H 4 ,4-NO 2 C 6 H 4 , 4-OHC 6 H 4 , 2-OHC 6 H 4 , 4-FC 6 H 4 , 2-CI-6-FC 6 H 3 ) or heterocyclic (2-SC 4 H 3 , 5-NO 2 -2-C 4 H 2 O) aldehyde to an equivalent amount of the appropriate 2-((4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-yl)thio)aceticohydrazide in the acetic acid medium. The study of physical-chemical properties of obtained compounds was carried out according to the methods outlined in SPU. Chromato-mass-spectral studies were performed on hazarding chromatograph Agilent 1260 Infinity HPLC equipped with mass spectrometer Agilent 6120 with ionization in electro-spray (ESI). Conclusion. This suggests the possibility for further study of biological action of the synthesized compounds. As a result of studies the N'-R 1 -eden-2-((4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-yl)thio)aceticohydrazides have been synthesized and their physical-chemical properties have been studied.

Introduction. In last decades considerable interest to the search of biologically active compounds in series of azole derivatives is indicated. This is mainly connected with the successful use of several drugs with heterocyclic system in the structure. Analysis of the pharmacological properties of heterocyclic nitrogen–containing compounds of the known groups let us to suggest, that the triazole substituent is an important pharmacophore fragment, responsible for the availability of diverse physiological activity. In addition, it causes a little toxicity. Considerable attention belongs to synthesis and research of the biological activity of 1,2,4-triazoles derivatives. The great importance also has research of the influence of heterocyclic fragments of different nature in combination in one molecule on the activity of the synthesized compounds. Like different synthons in the structure of 1,2,4-triazoles in various kinds of biological activity of the reaction products with an aim of new and highly efficient low-toxicity compounds reception. The aim of work was to study synthesis and properties of substances among salts of 2-(5-((theophylline-7'-yl)methyle)-4-phenyle-4 Н -1,2,4-triazole-3-ylthio)acetate acid. Materials and methods of the research . In the process as a starting material for reception of new series of compounds theophylline has been chosen. It is important to note, that by the diversity and strength of pharmacological effects, which appears, this structure takes its rightful place among heterocyclic compounds. Through the series of the successive stages 4-phenyle-5-(1',3'-dimethylxantine-7'-yl)methyle-1,2,4-triazole-3-thiol was obtained from the theophylline. Research of the physico-chemical properties of the received compounds conducted according to methods, described in the State Pharmacopoeia of Ukraine. open capillary method, elemental analysis (Elementar Vario L cube (CHNS)). 1 H NMR spectra of compounds were recorded with a spectrometer “Mercury 400” (solvent - DMSO-d 6 or DMSO-d 6 + CCl 4 , the internal standard - tetramethylsilane). Chromatography-mass spectral researches were performed on the instrument Agilent 1100 Series LC/MSD System, method of ionization - chemical ionization at the atmospheric pressure (APCI). Propyl ester of the theophylline-7-acetic acid. To the 0,055 mol of sodium hydrogencarbonate in 150 ml of DMF adds 0,05 mole of the theophylline and heated with stirring 5 - 10 minutes. To the reaction compound adds 0,055 mole of the monochloracetate acid propyl ester and boil with constant stirring 5 - 6 hours. After cooling to the reaction mixture with stirring, adds an equal volume of water. The precipitate dissolves, then falles again. Ester precipitate is filtered, washed with water, then with a small amount of methanol and dried. White crystalline solid, insoluble in water, soluble in organic solvents (alcohols, dioxane, DMF, DMSO). For the analysis is purified from 1-propanol. Yield 82%. Hydrazide of the theophylline -7-acetic acid. To the heated 0,03 mole solution of the propyl ester theophylline -7- acetic acid in 200 ml of ethanol adds 0.3 mole of hydrazine hydrate. Reactionary compound leave at room temperature for 12 hours. Hydrazide precipitate is filtered, washed with water, acetone and dried. Output 79%. White, amorphous substance, insoluble in water, acetone, soluble in alcohols, dioxane, soluble in DMF, DMSO. Crystallized from a mixture DMF-water (1:1). T m. = 210-211 oC. 2-(2-(theophylline-7'-yl)acetyl)-N-phenylhydrazinecarbothioamide . 0,05 mol of phenylisothiocyanate, 130 ml of dioxane and 90 ml of water heated up to boiling for 1 hour, cooled, add 100 ml of water, the precipitate is filtered, washed with water, 2-propanol and crystallized from a mixture water- dioxane, dimethylformamide. Output - 71 %. Tm . = 262-265 oC. 7-((5-mercapto-4-phenyl-4 H -1,2,4-triazoles-3-yl)methyl)theophylline . 0,01 mol of compound 2 -(2-(theophylline)acetyl)-N-phenylhydrazyncarbothio-amide, 0,01 mol of sodium hydroxide and 50 ml of water heated up to boiling during 2 hours, cooled and added to the filtrate 2 ml of concentrated hydrochloric acid. Output - 84%. Tm. > 270 o C. 2-((5-((theophylline-7'-yl)methyle)-4-phenyle-4 Н -1,2,4-triazole-3-il)thio)acetate acid . In a round, heat-resistant flack heated 0,01 mol of 7-((5-mercapto-4-phenyl-4 H -1 ,2,4-triazoles-3-yl) methyl)theophylline, 0,02 mol NaOH and 0,01 mol monochloracetate acid. Heated up to boiling for 1 h. Cooled. Neutralized by acetic acid. Output - 71%. Tm. = 227-230 o C. Salts of 2-(5-((theophylline-7'-il)methyle)-4-phenyle-4 Н -1,2,4-triazole-3-il-ti о )acetate acid . A compound: 0.01 mole of acetic acid, 35 ml of ethanol and 0.01 mol of corresponding base (monoethanolammonium, dyethylammonium, dyetanolammonium, monoetanolammonium, threebutylammonium, morpholine, piperidine, piperazine) heated for 1 hour in a water bath, the solvent is evaporated. Getting white crystalline substances soluble in water, soluble in diethyl ether and chloroform. For analysis compounds recrystallized from ethanol. Potassium, sodium salts of 2-(5-((theophylline-7'-il)methyle)-4-phenyle -4 Н -1,2,4-triazole -3-iltio)acetate acid. A compound - 0.01 mole of acetic acid and 0.01 mole of potassium or sodium hydroxide in 30 ml of water evaporated in a water bath. The dry residuum crystallized from ethanol. Getting white crystalline substances, difficulty soluble in organic solvents. For analysis compounds recrystallized from water. Magnesium , calcium, zinc , copper (II) and iron (II ) salts of 2-(5-((teophylline-7'-yl)methyle)-4-phenyle-4 Н -1,2,4-triazole-3-iltio)acetate acid . A compound of 0.02 mole acetic acid, 25 ml of water and accordingly 0.01 mol of magnesium oxide , calcium carbonate , zinc sulfate, copper ( II) sulfate or iron ( II) chloride is heated till the dissolution of precipitate , filtered , the filtrate evaporated. Received white, light blue , brown crystals with sharp melting points, little soluble in water, hardly soluble in organic solvents. For the analysis, compounds recrystallized from water. Ammonium salt of 2-(5-((teophylline-7'-yl)methyle)-4-phenyle-4 Н -1,2,4-triazole-3-iltio)acetate acid. A solution of 0.01 mole acetic acid in 30 ml of 25% ammonia solution evaporated. Received a white crystalline solid, easily soluble in water, difficult soluble in ethanol. For the analysis compound recrystallized from the compound - dioxane: water (3:1). Results and their discussion. As starting material we used 7 - ((5-mercapto-4-phenyl-4H-1 ,2,4-triazoles-3-yl) methyl) theophylline, received from 2 - (2 - (theophylline) acetyl)-N phenylhydrazyncarbotioamide, which was obtained from the previously described hydrazide theophylline-7-acetic acid as a result of interaction with phenylizotiocyanate. By interaction of the resulting thiol with monochloracetate acid in an aqueous solution of double lye number received the corresponding carboxylic acid. Research has shown, that the reaction proceeds quantitatively In the 1 Н NMR - spectra of the resulting acid was observed number of signals. In a strong part of magnetic field available the protons of -СН 2 -groups, which resonate as singlets at 3.90 m.p and 5.75 m.p The signals of СН 3 groups protons also appears as intense singlet in the 3.30 - 3.36 m.p region. Proton of the methyne group is characterized by a signal at 8.36 m.p. Signals of the phenyl radical protons in 1 Н NMR- spectra form two one - proton doublets (at 7.70 m.p. and at 7.48 m.p. ) and three one – proton triplets (at 6.83 - 7.17 m.p. ) . Broadening proton signal of aromatic COOH groups fixed at 12.0 m.p. IR- spectra of the received acid characterized by deformation and valence fluctuations of synthesized compounds basic fragments: plane deformation of C-H fluctuations in 1225 - 950 cm -1 area ( weak intensity band 1175-1125 сm -1 , 1110-1070 сm -1 , 1070-1000 1 сm -1 ), out – plane deformation of C-H fluctuations in the 1000-650 сm -1 area ( strong intensity band 770 - 730 сm -1 , , 710 - 690 сm -1 ). Available bands of the carboxyl group valence fluctuations - 1760 сm -1 . C = N in a 1660-1480 сm -1 cycle . Theophylline fragment: 3060 - 3010(ν с - н ), 1000 - 960 сm -1 (C- H deformation fluctuations), 875 - 775 сm -1 (C- H deformation fluctuations) , 1580 - 1520 сm -1 ( ring fluctation) . Also, available bands of NH- groups fluctuations within 1650 - 1620 сm -1 (ν as ) and 1345 - 1310 сm -1 (ν s ). Conclusions Installed the optimal conditions of salts reception

Metals in the form of nanoparticles are one of the long-term challenges for the creation of a new class of antibacterial agents. The biological activity of nanoparticles of metals depends directly on their physical and chemical properties. The objective of this work is to study the physicochemical parameters and antibacterial effects of copper nanoparticles for the standardization of the given nanomaterial during further use as an antibacterial agent. The physical and chemical parameters and antibacterial effects of copper nanoparticles are investigated. Optical methods, including atomic force microscopy, spectrophotometry, and fluorometry, are used to determine the sizes of associates of nanoparticles. The size of copper nanoparticles was 75 nm, and the sizes of nanoparticle associates are 481.1–1037 nm. An oxide film without any admixture of organic molecules is detected on the surface of nanoparticles. The antibacterial effects of copper nanoparticles are studied on the basis of clinical polyantibiotic-resistant strains of epidermal staphylococcus and gramnegative nonfermentative microorganisms (causative agents of purulent flammatory diseases among patients of traumatology and orthopedic in-patient hospital departments). As a result of the investigations, a clear antibacterial effect of copper nanoparticles with specified physical characteristics on gram-positive and gram-negative microorganisms of causative agents of wound infection is detected, which gives prospects for the further use of these particles as antibacterial agents.

The study has demonstrated that proapoptic concentrations of donors of NO (100 mmol SNP and 100 µmol NOC-5), H2S (10 mmol NaHS), and CO (50 µmol CORM-2) gases caused an increase in the intracellular level of active forms of oxygen in Jurkat cells. As this took place, the activation of redox-dependent transcription factor р53 was observed as Jurkat cells were exposed to 100 mmol SNP and 10 mmol NaHS. In the case of 100 µmol NOC-5 and 50 µmol CORM-2, an increase of р53 was not observed, but the expression of target gens of this transcription factor р21 (under the effect of NO and СО) and bax (under the effect of NO) increased. The antiproliferative concentration of hydrogen sulfide donor (50 µmol ) did not cause an increase in the intracellular production of active forms of oxygen and the activation of redox-dependent signal mechanisms.

The results of joint uranium and rhenium sorptions from the solutions with strong base anion exchange resin Ambersep A920U (herein after A920), are presented in the paper. Effect of salt form (sulfate, chloride, nitrate, hydroxide), nature of sulfate, nitrate, and chloride containing compounds (acids, their sodium and zinc salts), sodium carbonate and ammonium hydrocarbonate and their concentration in the solutions (1–1000 mol/m3) to sorption ability of the metals were studied in static conditions. It was found that А920 anionite sorb the metals from the solutions differently. Rhenium is sorbed with the anion exchange resin of all salt forms and from the solutions of any composition. The nature of sulfates (acid, salts) has different effects: sulfuric acid better suppresses rhenium sorption as compared to that for zinc and sodium sulfates. The increase of sulfate concentration from 1 to 1000 mol/m3 reduces sorption of rhenium gradually and steeply. The nature of nitrates and chlorides does not affect sorption ability of rhenium but high concentration of the compounds depresses its sorption. Rhenium sorption from carbonate and hydrocarbonate solutions proceeds similarly to that for sulfate solutions. Rhenium is sorbed better from sodium carbonate solutions than from ammonium hydrocarbonate solutions. Uranium is well sorbed with the anion exchange resin in sulfate form and badly with the anionite in nitrate and chloride forms. Uranium is sorbed only from sulfate, carbonate and hydrocarbonate solutions in contrary to rhenium. Sorption ability of uranium at concentrations from 1 to 1000 mol/m3 is growing in contrary to rhenium, however at higher concentrations sorption ability is declining similarly to that for rhenium. The following groups were registered in the IR-spectra of saturated anion exchange resin: SO42 −, HSO4−, NO3−, HCO3−, and CO32 − together with rhenium and uranium groups. Different sorption abilities of the metals were explained by their ion state in the solutions.

The purpose of the work was to study the antimicrobial activity of 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts by "hanging drop" and “serial dilution” methods in broth (limiting concentration option) and establish some patterns of "structure – action" depending. Materials and methods. The objects of research were 9 new compounds of 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts. These compounds are the crystal substances which are odorless, soluble in water and organic solvents. To achieve a more objective picture of the research we applied two methods: "hanging drop" and “serial dilution” in broth (limiting concentration option). To study the effectiveness of substances we used the test cultures of E. coli , Salmonella typhymurium , Staphylococcus epidermidis, P. aeruginosa . Results and discussion. In the study we have found that 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts can differently inhibit the growth of test cultures. The results show that the data obtained by two methods correlated with each other. Thus, the 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts are active against most strains of E. Coli . and Salmonella typhymurium . Analyzing the impact of 2-((4-R-3-(morfolinomethylene)-4 H -1,2,4-triazole-5-yl)thio) acetic acid salts we have noted that the replacement of the phenyl radical (PKR-135, 139) on the free amino group at N4 nitrogen of 1,2,4- triazole cycle (PKR-173, 177) leads to the disappearance of antimicrobial activity against the studied strains. It was established that the transition from morfolin cation (PKR-133) to the piperydyn cation (PKR-134) in the molecules of 2-((4-phenyl-3-(morfolinometylen)-4 H -1,2,4-triazole-5-yl) thio) acetic acid is accompanied by a significant increase in antimicrobial effect. It was interesting that among all the cations in the molecules of 2-((4-amino-3-(morfolinometylen)-4H-1,2,4-triazole-5-yl) thio) acetic acid salt (PKR-173, 174, 177, 234) only the presence of sodium cation (PKR-174) leads to a pronounced antimicrobial effect against studied strains. Conclusions. The study had found that the most effective in relation to the main groups of pathogenic bacteria are substances PKR-134, 135, 136, 139 and 174. Certain regularities based on "structure-action" have been established, this information can be integrated into future targeted search of substances with antimicrobial properties.

Publications of domestic and foreign scientists in the last ten years clearly show that the search for new molecules among 1,2,4-triazole furan derivatives has not only theoretical interest in the study of physical and chemical properties of compounds, but also has a practical significance on the implementation of the most active agents in various spheres of human activity. The most striking example is the registration of new domestic veterinary drug «Tryfuzol 1% solution for injections» (registration certificate AB-05486-01-14 from 01.10.2014). Active substance of the «Tryfuzol» is a water-soluble substance, which is furan derivative of 1,2,4-triazole-3-thione according to the chemical formula. Aim. Further research of reactions which are related to the study of physical and chemical properties of new 1,2,4-triazole-3-thione derivatives with heterocyclic furan system fragments, is an important task in the search for new biologically active compounds needed for the potential drugs creation. Methods and results. For the first time we have synthesized the number of 4-amino-5-(furan-2, 2-metylfuran-3-yl)-1,2,4-triazole-3-thiol alkyl derivatives. As alkylating agents we have used appropriate bromalkans. Conclusions. The structure of the synthesized compounds has been confirmed by complex physical and chemical analysis methods (elemental analysis, NMR spectroscopy, chromatography-mass spectrometry), and their individuality has been confirmed chromatographically.

Производные 1,2,4-триазола получили большое применение в медицинской практике благодаря широкому спектру биологического действия и низкой токсичности, что, в свою очередь, обусловлено присутствием в их структуре триазольного цикла. Именно поэтому данный класс органических гетероциклических соединений является особенно интересным и перспективным для исследования его физико-химических и биологических свойств. С целью поиска новых потенциально биологически активных веществ было синтезировано 13 новых соединений, ранее не описанных в научной литературе, – 3-(4-(трет-бутил)-фенил)-5-(R-илтио)-4H-1,2,4-триазол-4-аминов, а также предложены препаративные методы их синтеза. Структура новых соединений была изучена с помощью современных инструментальных методов анализа (хромато-масс-спектрометрия, ИК, 1Н ЯМР-спектроскопия и элементный анализ). Установлено, что результаты исследований подтверждают структуру данных соединений. Это свидетельствует о возможности их дальнейшего применения в биологических исследованиях., Aim. 1,2,4-triazole derivatives are widely used in medical practice due to its wide range of biological effect and small toxicity. This fact makes this class of organic heterocyclic compounds especially interesting and promising for the study of their physical-chemical and biological properties. Thirteen novel compounds, namely 3-(4- (tert-butyl)phenyl)-5-(R-ylthio)-4H-1,2,4-triazole-4-amines, that were not previously described in the literature, have been synthesized with the aim of search for new potentially biologically active compounds.Methods and results. In order to create new biologically active compounds 13 novel 3-(4-(tert-butyl)phenyl)-5-(R-ylthio)-4H-1,2,4-triazole-4-amines have been synthesized, preparative methods of their synthesis have been proposed, the structure of synthesized compounds has been confirmed by IR-, 1H NMR-spectroscopy, chromatography-mass spectrometry and elemental analysis. In addition, the compounds have been tested for antimicrobial and antioxidative activities.Conclusions. A preparative methods of synthesis of 3-(4-(tert-butyl)phenyl)-5-(R-ylthio)-4H-1,2,4-triazol-4-amines that can be used for chemical modeling of new biologically active compounds are described. The structure of the synthesized compounds was confirmed by complex of modern methods of investigation, namely: IR-, 1H NMR-spectroscopy, chromatography-mass spectrometry and element analysis.This indicates the possibility of using these substances to further biological studies., Похідні 1,2,4-тріазолу отримали широке застосування в медичній практиці завдяки різноманітному спектру біологічної дії та низькій токсичності. Саме тому цей клас органічних сполук є особливо цікавим і перспективним для дослідження його фізико-хімічних, біологічних властивостей. З метою пошуку нових потенційно біологічно активних речовин синтезували 13 нових сполук, котрі не були описані раніше в науковій літературі, – 3-(4-(трет-бутил)феніл)-5-(R-ілтіо)-4H-1,2,4-тріазол-4-амінів, а також запропонували препаративні методи їхнього синтезу. Структуру нових речовин вивчили за допомогою сучасних інструментальних методів аналізу (хромато-мас-спектрометрія, ІЧ-, 1Н ЯМР-спектроскопія та елементний аналіз). Встановили: результати роботи підтверджують структуру цих сполук, що свідчить про можливість надалі їх застосовувати в біологічних дослідженнях.

The investigation results showed carbon monoxide had antiproliferate potential in Jurkat cells. This gaseous transmitter led to delay of G1 phase of cell cycle. Inhibition of p38 MAPK-dependent pathways didn’t influence on CO-mediated proliferation of Jurkat cells changes.

In this study we have investigated the effect of reactive oxygen species produced by some chemicals in aqueous solutions on activity of adenosine deaminase 2 (ADA2) purified from human blood plasma. An activating effect on ADA2 was observed in vitro with sodium nitroprusside (SNP), the source of NO (nitrosonium ions NO(-) in aqueous solutions). Not SH-groups of cysteine but other amino acid residues sensitive to NO were responsible for ADA2 activation. The SNP-derived activation was more pronounced when purified ADA2 was preincubated with heparin and different proteins as an experimental model of the protein environment in vivo. The most effective was heparin, which is known for its ability to regulate enzyme and protein functions in extracellular matrix. We conclude that ADA2 is a protein with flexible conformation that is affected by the protein environment, and it changes its activity under oxidative (nitrosative) stress.

The effect of the cattle cord blood low-molecular fraction (up to 5 kDa) (FCB) on regeneration of knee joint cartilage following mechanical injury was studied in rats using biochemical, histological and roentgenological methods. It was shown that intramuscular injection of FCB significantly stimulated the accumulation of the basic components of matrix, the most important structural proteins in cartilage regeneration as well as provided the positive effect on morphologic state of cartilage and surrounding tissues. That positive effect was noted during both stage of granulation and stage of chondrocyte development. It was shown that injection of FCB promoted normalization of motor activity in injured limb.

Until recent time it has seemed obvious that suppressive function in the immune system is provided by one subpopulation of Tlymphocytes-suppressors. At present it is usually considered that regulatory cells (T-reg) are key cells-suppressors of the immune response. There exist two main mechanisms of T-reg immunosuppression realization: direct (when there is direct contact between cells) and distant (cytokine-dependent). For suppression of the immune response Т-reg cells produce cytokines with suppression activity: TGF-β, IL-10, IFN-γ, IL-35. Meanwhile the increasing number of facts indicates that suppression of the immune response is a multi-component process. A considerable role in suppression of the immune response is assigned to the endocrine system. However, immunosuppression mechanisms under infection, neoplastic processes and the influence of xenobiotics on the organism are not completely clear.

Results of the antihypoxic activity of salts of 2-(5- (adamantane-1-yl)-4 H -1,2,4-triazole-3-ylthio) acetate acid are given in the article. Promising for further studies of the biological activity of the synthesized compounds were proved.

We have studied the calcium consumption by nursing mothers and children from risk groups on decreased mineral bone density in different age periods under conditions of Tomsk. The calcium content in breast milk in the first six month of lactation was determined by the method of instrumental neutron-activation analysis. It has been found that the calcium consumption by the most nursing mothers corresponded to physiological norms. In the lactation dynamics, the calcium content in the breast milk decreased at the third month and increased at the sixth month of lactation. The average calcium consumption was (834,3 ± 132,3) mg in children aged of 1—3 and (959,0 ± 99,5) mg/day in children of 4—6 years old. Among schoolchildren, the average calcium consumption was (860,3 ± 98,2) mg/day in the age of 7—10 and (777,9 ± 59,3) mg/day in eth age of 11—18. It is 1,2—1,6 times lower than the recommended norm. In teenagers, the calcium deficit in food is more often compared to preschool children.

Apoptosis of blood neutrophils from healthy donors was studied under conditions of cell culturing with different concentrations of H(2)O(2), selective NO synthase inhibitor, and inductor of NO synthesis (L-arginine). In vitro incubation of neutrophilic leukocytes with 5 mM H(2)O(2) led to activation of the apoptotic program in neutrophils, which was seen from increased content of Bax protein in the cells and increased number of apoptotic cells in the culture. Increased content of annexin-positive cells after incubation of neutrophil culture with NO synthase inhibitor suggests involvement of NO in the regulation of neutrophil apoptosis under conditions of oxidative stress, while L-arginine prevented H(2)O(2)-induced programmed cell death.

The aim of study was to investigate diuretic activity of 1,2,4-triazole derivatives which contain С5 atom 5-bromfuran-2-yl substituent in the 1,2,4-triazole nucleus, and to establish interrelation between chemical structure and diuretic action of 1,2,4-triazole derivatives. Methods and results. For the investigation of the diuretic activity were used 15 compounds, namely 3-(5-bromofuran-2-yl)-4-R-(4H)-1,2,4-triazole-5-thiones, their S-derivatives and 2-(5-bromofuran-2-yl)-5-R'-thiazolo[3,2-b][1,2,4]triazole-6(5H)-ones. During the study Ye. B. Berkhin’s method has been used to establish the influence of the compounds on the renal excretory function. Conclusion. The most active substance among 1,2,4-triazole derivatives was morpholinium 2-((5-bromofuran-2-yl)-4-ethyl-1,2,4-triazole-3-ylthio)acetate.

Aim. To study biological properties of the compounds formed by the combination of the 1,2,4-triazoles, furans and other functional substitutes. Methods and results. It is known that 1,2,4-triazole heterocyclic system is promising for creation of new biologically active molecules. The entire series of drugs, the active ingredient of which is a derivative of the 1,2,4-triazole (fluconazole, ribavirin, avesstim, trifuzol and others) has entered in the practice of modern medicine, pharmacy and veterinary medicine. Special attention to the creation of potential drugs deserves the opportunity of combining fragments of 1,2,4-triazole, the "nucleus" of furan and other substitutes. Literary sources show different types of pharmacological activity of the compounds formed by such "symbiosis". Subsequent chemical transformations of these structures contribute to the establishment of consistent pattern between the structure and biological activity of the corresponding 1,2,4-triazole derivatives, and this in turn has positive effect on the most rapid identification of the most promising classes of compounds. Conclusion. Despite the huge number of publications devoted to the study of the biological properties of the 1,2,4-triazole derivatives with furan fragment, there is no systematization of the results of these research.

Здійснили дослідження протимікробної та протигрибкової активності серед S-похідних 7-((3-тіо-4-R-4Н-1,2,4-тріазол-3-іл)метил)теофіліну. Як набір стандартних тест-штамів взято Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomоnas aeruginosa ATCC 27853, Candida albicans ATCC 885-653. Встановили, що найбільш активними серед сполук, що одержали, є алкілпохідні 7-((3-тіо-4-R-4Н-1,2,4-тріазол-3-іл)метил)теофіліну. Серед синтезованих солей привернув увагу амоній 2-(5-((теофілін-7-іл)метил)-4-феніл-4Н-1,2,4-тріазол-3-ілтіо)ацетат, який виявився активним стосовно Staphylococcus aureus. Визначили перспективний клас сполук для наступних досліджень за цим видом біологічної активності., Aim. The research of antimicrobial and antifungal activity of 7-((3-thio-4-R-4H-1,2,4-triazoles-3-yl)methyl)theophylline S-derivatives has been erformed.Methods and results. Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomоnas aeruginosa ATCC 27853, Candida albicans ATCC 885-653 have been taken as a set of standard test-strains. It has been proved that the most active alkyl-derivatives are 7-((3-thio-4-R-4H-1,2,4-triazole-3-yl)methyl)theophylline. Among the synthesized salts, which turned to be active against Staphylococcus aureus, the 2-(5-((theophylline-7-yl)methyl)-4-phenyl-4H-1,2,4-triazole-3-ylthio)acetate ammonium has attracted our attention.Conclusion. The perspective class of compounds for further research on this type of biological activity has been defined., Проведены исследования противомикробной и противогрибковой активности среди S-производных 7-((3-тио-4-R-4Н-1,2,4-триазол-3-ил)метил)теофиллина. В качестве набора стандартных тест-штаммов взято Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomоnas aeruginosa ATCC 27853, Candida albicans ATCC 885-653. Установлено, что наиболее активными среди полученных соединений являются алкилпроизводные 7-((3-тио-4-R-4Н-1,2,4-триазол-3-ил)метил)теофиллина. Среди синтезированных солей наибольшее внимание привлек аммоний 2-(5-((теофиллин-7-ил)метил)-4-фенил-4Н-1,2,4-триазол-3-илтио)ацетат, который оказался активным по отношению к Staphylococcus aureus. Определён перспективный класс соединений для дальнейших исследований по данному виду биологической активности.

В создании оригинального препарата основную роль играет подбор, синтез и установление биологических свойств нового соединения. C целью поиска новых биологически активных соединений были синтезированы 3-(алкилтио)-4-R-5-(тиофен-2-илметил)-4H-1,2,4-триазолы, где R – метил, этил, фенил, реакцией алкилирования 4-R-5-(тиофен-2-илметил)-4H-1,2,4-триазол-3-тиолов галогеналканами (1-бромбутаном, 1-бромпентаном, 1-бромгексаном, 1-бромгептаном, 1-бромоктаном, 1-бромнонаном, 1-бромдеканом) в среде н-бутанола и изучены их физико-химические свойства современными физико-химическими методами анализа: элементного анализа, ИК-спектроскопии, а их индивидуальность – методом ВЭЖХ-МС. Это свидетельствует о возможности дальнейшего изучения биологического действия синтезированных соединений., Aim. Selection, synthesis and biological properties of new compound play major role in creating original medicines.Methods and results. Therefore, to find new bioactive compounds 3-(alkylthio)-4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazoles, where R - methyl, ethyl, phenyl, have been synthesized, by alkylation reaction of 4-R-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thiols with 1-bromobutane, or 1-bromopentane, or 1-bromohexane, 1-bromoheptane, 1-bromooctane, 1-bromononane, 1-bromodekane in the n-butanol medium and their physical-chemical properties have been studied using modern physical-chemical methods of analysis, elemental analysis, IR spectroscopy, and their individuality using HPLC-MS.Conclusion. This suggests the possibility of further studying the biological effect of the synthesized compounds., У створенні оригінального препарату основну роль відіграє підбір, синтез і встановлення біологічних властивостей нової сполуки. З метою пошуку нових біологічно активних сполук було синтезовано 3-(алкілтіо)-4-R-5-(тіофен-2-ілметил)-4H-1,2,4-тріазоли, де R – метил, етил, феніл, реакцією алкілування 4-R-5-(тіофен-2-ілметил)-4H-1,2,4-тріазол-3-тіолів галогеналканами (1-бромбутаном, 1-бромпентаном, 1-бромгексаном, 1-бромгептаном, 1-бромоктаном, 1-бромнонаном, 1-бромдеканом) у середовищі н-бутанолу та вивчено їхні фізико-хімічні властивості сучасними фізико-хімічними методами аналізу: елементного аналізу, ІЧ-спектроскопії, а їх індивідуальність – методом ВЕРХ-МС. Це свідчить про можливість надалі вивчати біологічну дію синтезованих сполук.