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A convenient method for the obtaining of 3,6-diaryl-1,2,4-triazines substituted with residues of higher alcohols in the position of C5 via the ipso-substitution of cyano group in under the solvent free conditions was reported. This method indicates a new example for the functionalization of the 1,2,4-triazines via the substitution of the cyano group.

Rationale. The reference material of composition with the established metrological characteristics including a certified value and an expanded uncertainty is necessary to ensure an effective accuracy and precision control of results of element composition determination in food ingredients and products. This paper represents the development of a reference material of food crop composition for selenium, nitrogen, phosphorus and potassium content. Methods. To identify the selenium the hybrid atomic absorption method was used, to identify the nitrogen and phosphorus the photometric method was used, to determine the potassium flame-photometric method was used. When determining the metrological characteristics of the reference material the Russian national instructions and recommendations MI 3174-2009 and P 50.2.058-2007 were applied. Results. Based on the research findings the reference material of Chinese cabbage composition with a certified value and an expanded uncertainty was developed: for selenium 0.044 ± 0.017 mg/kg; for nitrogen 4.09 ± 0.27 %; for phosphorus 0.69 ± 0.14 %; for potassium 2.87 ± 0.22 %.

Two mutually complementary synthetic approaches towards 3- and 3,4-disubstituted 1-(2-pyridyl) isoquinolines were studied. The aryne-based method was successfully used for the obtaining of the corresponding the 3-cyano-1-(2-pyridyl)isoquinolines in one step/pot reaction, while it is unacceptable for the obtaining of other 1-(2-pyridyl)isoquinolines. The enamine-based approach was successfully applied for the synthesis of other 1-(2-pyridyl)isoquinolines, while it was unacceptable for the obtaining of 3-cyano-1-(2-pyridyl)isoquinolines.

Background: Cerebral aneurysms (CA) are a widespread vascular disease affecting 50 per 1000 population. The study of the influence of histological, morphological and hemodynamic factors on the status of the aneurysm has been the subject of many works. However, an accurate and generally accepted relationship has not yet been identified. Methods: In our work, the results of mechanical and spectroscopic measurements are considered. Total investigated 14 patients and 36 their samples of CA tissue. Results: The excitation–emission matrix of each specimen was evaluated, after which the strength characteristics of the samples were investigated. Conclusions: It has been shown that there is a statistically significant difference in the size of the peaks of two components, which characterizes the status of the aneurysms. In addition, a linear regression model has been built that describes the correlation of the magnitude of the ultimate strain and stress with the magnitude of the peaks of one of the components. The results of this study will serve as a basis for the non-invasive determination of the strength characteristics of the cerebral tissue aneurysms and determination of their status.

The cultivation of plants in the form of callus cultures constitutes a renewable source of secondary plant metabolites. The conditions for the cultivation of callus cultures affect the yield of target compounds. Callus cultures of Hyssopus officinalis were chosen for study. Nutrient media of various compositions were used for Hyssopus officinalis callus culture. For each culture, data on the quantitative contents of saponins, flavonoids and polyphenolic compounds, as well as antioxidant activity, were obtained. It was found that Murashige and Skoog medium supplemented with 1-naphthylacetic acid and kinetin led to the highest yield of secondary metabolites.

This work aims to study the qualitative composition of biologically active substance (BAS) extracts in vitro callus, cell suspension, and root cultures of the medicinal plant Rhaponticum carthamoides. The research methodology is based on high-performance liquid chromatography, and 1H nuclear magnetic resonance (NMR) spectra, to study the qualitative and quantitative analysis of BAS. The results of the qualitative composition analysis of the dried biomass extracts of in vitro callus, cell suspension and root cultures showed that the main biologically active substances in the medicinal plant Rhaponticum carthamoides are 2-deoxy-5,20,26-trihydroxyecdyson (7 mg, yield 0.12%), 5,20,26-trihydroxyecdyson 20,22-acetonide (15 mg, yield 0.25%), 2-deoxy-5,20,26-trihydroxyecdyson 20,22-acetonide (6 mg, yield 0.10%), 20,26-dihydroxyecdyson 20,22-acetonidecdyson 20,22-acetonide (5 mg, yield 0.09%), and ecdyson 20,22-acetonide (6 mg, yield 0.10%). In the future, it is planned to study the antimicrobial, antioxidant, and antitumor activity of BAS of extracts of in vitro callus, cell suspension, and root cultures of the medicinal plant Rhaponticum carthamoides, for the production of pharmaceuticals and dietary supplements with antitumor, antimicrobial and antioxidant effects.

Plants of the Miscanthus genus (Miscanthus Anderss.) have a unique index of biomass production in relation to the occupied area. Miscanthus plants can be attributed to promising second-generation raw materials for the production of bioethanol and biofuel. Miscanthus plants are characterized by a high cellulose content. Herein, we report the results of a study on the obtained delignified cellulose with subsequent processing into bioethanol using microbial communities. In the course of the study, the optimal conditions for the delignification of the initial plant material for cellulose were selected. Ethanol with a high degree of conversion was successfully obtained from the isolated delignified cellulose. The article describes the pilot technological scheme for the conversion of Miscanthus plant biomass to bioethanol involving the delignification stages, followed by the conversion of the resulting cellulose into bioethanol by a consortium of microorganisms. As a result of the study, it was found that delignification using trifluoroacetic acid leads to the production of cellulose of high purity. Bioethanol with a yield of 3.1% to 3.4% in terms of the initial amount of biomass was successfully obtained by a microorganism consortium of Saccharomyces cerevisiae M Y-4242/Pachysolen tannophilus Y-3269, and Scheffersomyces stipitis Y-3264.

Traumatic brain injury (TBI) often causes massive brain cell death accompanied by the accumulation of toxic factors in interstitial and cerebrospinal fluids. The persistence of the damaged brain area is not transient and may occur within days and weeks. Chaperone Hsp70 is known for its cytoprotective and antiapoptotic activity, and thus, a therapeutic approach based on chemically induced Hsp70 expression may become a promising approach to lower post-traumatic complications. To simulate the processes of secondary damage, we used an animal model of TBI and a cell model based on the cultivation of target cells in the presence of cerebrospinal fluid (CSF) from injured rats. Here we present a novel low molecular weight substance, PQ-29, which induces the synthesis of Hsp70 and empowers the resistance of rat C6 glioma cells to the cytotoxic effect of rat cerebrospinal fluid taken from rats subjected to TBI. In an animal model of TBI, PQ-29 elevated the Hsp70 level in brain cells and significantly slowed the process of the apoptosis in acceptor cells in response to cerebrospinal fluid action. The compound was also shown to rescue the motor function of traumatized rats, thus proving its potential application in rehabilitation therapy after TBI.

На локальной математической модели церебральной артериовенозной мальформации (АВМ), состоящей из набора трубок различного диаметра, рассматриваются различные сценарии ее эмболизации. Показано, что наименьший перепад давления на входе в АВМ достигается в случае эмболизации на первом этапе наиболее широкой фистулы, затем крупного и мелкого компартментов мальформации. Проводится сравнение модельных расчетов с результатами эмболизации АВМ у 15 пациентов.

Впервые проведены измерения скорости и давления крови в артериях головного мозга до четвертых сегментов при наличии артериовенозных мальформаций и артериальных аневризм. Разработан и внедрен аппарат диаграмм давление - скорость и расход - поток энергии, позволяющий характеризовать тип сосудистой аномалии по гемодинамическим параметрам и отслеживать эффективность операции. На основании вейвлет-анализа локальных гемодинамических параметров в пораженных и здоровых ветвях артерий обнаружено изменение низкочастотной части спектра кровотока после операции. Полученные результаты дают качественные и количественные признаки аномалии сосудов головного мозга и позволяют оценить эффективность эмболизации в процессе операции.

Triazolo[5,1-b]purines are rare structural analogues of natural nucleosides and nucleobases purine series. At the same time, prominent representatives of azolopurines exhibit a broad spectrum of antiviral effect, activity against of rheumatoid arthritis, psoriasis, Alzheimer's, Parkinson's and etc. Despite the practical value azolo[5,1-b]purines extremely sparingly represented in the chemical literature, due to the complexity of their synthesis. We suggest a convenient way to synthesize triazolopurines with aminotriazolo[1,5-a]pyrimidines (2) as available starting compounds obtained in good yield by reduction of nitro derivatives (1).

New analogues of acyclovir have been prepared by reacting 1,2,4-triazolo[1,5-a]pyrimidin-7-ones 1а-i and (2-acetoxyethoxy)methyl acetate 2 in the presence of trimethylsilyl trifluoromethanesulfonate as a catalyst. Thei nteraction between the compounds 1а-е and 2 has led to a mixture of N3 and N4 isomers. In contrast, the reaction of compounds 1g-i and 2 proceeded selectively to form N3 isomers. In the case of compounds 1a-c the predominant product is the one with the acyclic moiety in azine ring (N4 isomer). Interaction between 1d-f and 2 has led to mixtures comprising mainly N3 isomer. It has been found that the ratio of glycosylation products 1 and 2 are thermodynamically controlled. The structure of the obtained compounds has been proved by 1Н, 13С, two-dimensional 1Н-13С NMR spectroscopy and X-ray analysis.

The aim of the present study was to examine how administration of a compound of 1,3,4- thiadiazine class 2-morpholino-5-phenyl-6H-1,3,4-thiadiazine, hydrobromide (L-17) with hypothermia inducing properties affects the brain metabolism. The mechanism by which L-17 induces hypothermia is unknown; it may involve hypothalamic central thermoregulation as well as act via inhibition of energy metabolism. We tested the hypothesis that L-17 may induce hypothermia by directly inhibiting energy metabolism. The study in vivo was carried out on Sprague-Dawley adult rats. Two doses of L-17 were administered (190 mg/kg and 760 mg/kg). Brain metabolites were analyzed in control and treated groups using magnetic resonance spectroscopy, along with blood flow rate measurements in carotid arteries and body temperature measurements. Further in vitro studies on primary cultures from rat hippocampus were carried out to perform a mitochondria function test of L-17 pre-incubation (100 μM, 30 min). Analysis of brain metabolites showed no significant changes in 190 mg/kg treated group along with a significant reduction in body temperature by 1.5°C. However, administration of L-17 in higher dose 760 mg/kg provoked changes in brain metabolites indicative of neurotoxicity as well as reduction in carotid arteries flow rate. In addition, a balance change of excitatory and inhibitory neurotransmitters was observed. The L-17 pre-incubation with cell primary cultures from rat brain showed no significant changes in mitochondrial function. The results obtained in the study indicate that acute administration of L-17 190 mg/kg in rats induces mild hypothermia with no adverse effects onto brain metabolism.