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We have designed and synthesized a new series of amide derivatives of thiazolo[5,4-d]pyrimidines (10a-j) and their structures were characterized by 1H NMR, 13C NMR and mass spectral data. Furthermore, all compounds were evaluated for in vitro cytotoxicity effects against four human cancer cell lines such as PC3 (prostate cancer), A549 (lung cancer), MCF-7 (breast cancer) and DU-145 (prostate cancer) by employing MTT assay. The cytotoxicity effects of the amide derivatives (10a-j) were compared with etoposide utilized as the positive control. Among them, five compounds 10a, 10b, 10c, 10h and 10j possessed significant cytotoxicity properties as compared with etoposide. [ABSTRACT FROM AUTHOR]

Urease is a dinickel enzyme that is responsible for the hydrolysis of urea to ammonia and carbon dioxide. A series of bacteria like Helicobacter pylori produce urease in order to release ammonia via urea hydrolysis and survive in acidic environments. Urease inhibitors are often used as a part of the medical treatment of infections by ureolytic bacteria. In this work, a series of diaryl pyrimidine derivatives (compounds 6a–6i) have been synthesized as urease inhibitors, their inhibitory activities against Jack bean urease have been investigated in vitro, and the obtained values of IC50 showed potent urease inhibitory activity. Cytotoxic activity of the synthesized compounds was evaluated against four cell lines (HT-29, MCF-7, T47D, and NIH3T3). Many of the tested compounds did not show significant cytotoxicity, and compounds 6d, 6g, and 6i did not show any cytotoxic activity against these cell lines. Among these, compound 6d showed the most pronounced urease inhibitory activity (IC50 = 780 ± 50nM), being over 28-fold more potent than thiourea (IC50 = 22.01 ± 0.08 ìM) and 128-fold more potent than hydroxyurea (IC50 = 100.00 ± 0.08 ìM) as standard inhibitors, respectively. The results of molecular docking studies showed that compound 6b had the best binding energy and exhibited proper interaction with the active site of urease. [ABSTRACT FROM AUTHOR]

In this study, a new benzopyrimidine analog was designed and synthesized by substituting 3-nitrophenyl ring and thiosemicarbazide nucleus at N-3 and C-2 positions of quinazoline ring, respectively. The title compounds, 1-substituted-3-(3-(2-chlorophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)isothioureas 7A – 7J were obtained via reactions of 2-hydrazino-3-(2-chlorophenyl)quinazolin-4(3H)-one (5) with different alkyl/aryl isothiocyanates followed by methylation with dimethyl sulphate. All synthesized compounds were screened for their antitubercular, anti-HIV, and antibacterial activity against selected Gram-positive and Gram-negative bacteria using agar diffusion method. Amongst, compounds 2-methyl-3-(3-(2-chlorophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)-1-(3-chloropheny)isothiourea (7I) and 2-methyl-3-(3-(2-chlorophenyl)-4-oxo-3,4-dihydrobenzopyrimidin-2-ylamino)-1-(3-chlorophenyl)isothiourea (7F) showed the most potent activity against P. vulgaris and S. aureus with a MIC of 3 μg/mL. Compound 7I exhibited antitubercular activity at a minimum MIC of 3.125 μg/mL and anti-HIV activity at EC50 of 2.91 μg/mL against HIV1 and HIV2, thus offering probable lead for further development and optimization of new antitubercular and anti-HIV drugs. Results obtained in this study confirm that the synthesized and biologically evaluated benzopyrimidines possess promising antimicrobial, antitubercular, and anti-HIV properties and provide new scaffolds for antimicrobial activity. [ABSTRACT FROM AUTHOR]

The pyrimidine scaffold is a versatile lead heterocycle in pharmaceutical development. It has diverse chemical reactivity, accessibility and a wide range of biological activities. In the past few years, the pyrimidine derivatives have been developed drastically as potent anticancer agents. This review highlights the current status of pyrimidine molecules in cancer therapy. The in vivo models have been enumerated for the specific types of cancer. The structure – activity relationship (SAR) of fused and substituted pyrimidine derivatives for anticancer activity is discussed. Electron withdrawing groups on aryl moiety attached to both substituted and fused pyrimidine influenced positively, and enhanced potency of novel small molecules as anticancer agents. Electron donating groups reduced the antiproliferative activity. Thus, scientists and researchers of medicinal chemistry discipline could design small molecules with a pyrimidine scaffold possessing more promising anticancer potential. [ABSTRACT FROM AUTHOR]

New condensed pyrimidine compounds with a benzoannelated quinazoline structure and various functional substituents at the pyrimidine N3-position were synthesized and included 2-methyl-3-(2-phenyl-2-oxoethyl) quinazolin-4(3H)-one; 3-(2-tert-butyl-2-oxoethyl)quinazolin-4(3H)-one; 3-[2-(1-naphthyl)-2-oxoethyl]-6-bromoquinazolin-4(3H)-one; 3-(2-isopropyloxy-2-oxoethyl)quinazolin-4(3H)-one; and 3-{2-[(4,6-dimethylpyrimidin- 2-yl)amino]-2-oxoethyl}quinazolin-4(3H)-one. The new quinazoline derivatives were found to produce a corrective action on proliferation processes in immunocompetent organs as manifested by restoration of the number of splenocytes and thymocytes on the background of cyclophosphan-induced immunosuppression in CBA mice of both sexes aged 3 – 4 months. [ABSTRACT FROM AUTHOR]

2-Oxo-2,5,6,7-tetrahydro-3-cyano-1H-cyclopenta[b]pyridine was used as the starting point to develop an accessible synthesis of condensed cyclopentanopyrido[3',2':4,5]thieno[3,2-d]pyrimidine derivatives. The neurotropic activity of these compounds was studied, and a number of them showed anticonvulsant activity as antagonism to corasol. Compound II, like diazepam, had anti-anxiety and activating effects, while the other compounds had sedative activity. [ABSTRACT FROM AUTHOR]

A series of twenty molecules based on thienopyrimidine nucleus fused with 5-, 6-, and 7-membered lactam rings as well as triazole were synthesized via 4-step reactions. The target compounds were obtained in good yield and confirmed for their structural integrity. The cytotoxic activity against A431 human epidermoid carcinoma and H9c2 rat cardiomyocyte cells were studied by MTT assay. Most of the synthesized compounds except 8a showed 85% cell death in both human A341 and rat H9c2 cell lines, indicating potential anticancer activity of these compounds. Interestingly, compound 8a showed a reversal in trend by enhancing the growth of both A341 and H9c2 cells. [ABSTRACT FROM AUTHOR]

With evident biological importance, a new series of pyrazolo[3,4-d]pyrimidines 3a,3b and 4a,4b were synthesized via the formation of pyrazol-3-one 2a and 2b substrates. All compounds were evaluated for in vitro cytotoxic activity against MCF-7 (breast adenocarcinoma) and A549 (lung cancer) cell lines. The obtained results showed that pyrazolo[3,4-d] pyrimidin-4-ol 3a bearing phenyl group at N-1 and p-C6H4 at C-6, and 4b with dinitrophenyl at N-1 and furanyl moiety at C-6 had better inhibitory activity against MCF-7 with IC50 values in a micromolar range as compared to other substrates. The synthesized compounds can be considered as new candidates for further optimization as anticancer agents. [ABSTRACT FROM AUTHOR]

Aseries of dihydrotetrazolo[1,5-a]pyrimidine derivatives were synthesized via a three-component reaction of benzoylacetone with aromatic aldehydes and 5-aminotetrazole monohydrate. The obtained compounds were tested for analgesic activity using the acetic acid-induced writhing test. Their acute toxicities were determined. (7-Aryl-5-methyl-4,7-dihydrotetrazolo[1,5-a]pyrimidin-6-yl)(phenyl)methanones were found to exhibit analgesic activity comparable to that of the reference drug metamizole sodium and were low-toxicity compounds. The obtained results were indicative of good prospects for further investigation of analgesic properties in this series of compounds. [ABSTRACT FROM AUTHOR]

A series of quaternary salts were obtained by reacting 3-(4-bromoacetylphenyl)-1-methylquinolin-2(1H)-one with Py, 4-methylpyridine, quinoline, benzo[f]quinoline, and triphenylphosphine. Derivatives of thiazole, imidazo[1,2-a]pyridine, and imidazo[1,2-a]pyrimidine were produced using dinucleophilic reagents. Several of the synthesized compounds possessed high antimicrobial activity, indicating that further research on this series of compounds was promising. [ABSTRACT FROM AUTHOR]

The logical framework approach was implemented for designing CNS-active N-substituted 1 H-pyrimidin-4-ones. Formation energies of possible ligand-receptor complexes with D-dopamine and GABA Receptors were determined from molecular docking calculations. The results allowed the probability of psychotropic activity manifesting in the modeled compounds to be estimated. The most promising compounds were prepared by a modified synthetic procedure. The effect of the heteroatom type in N-heterocyclic 1 H-pyrimidin-4-ones on the product yield was studied. Compounds I - IV and VI at a dose of 50 mg/kg exhibited anticonflict activity. The mercaptotriazole derivative of pyrimidin-4-one had the greatest anticonflict activity. [ABSTRACT FROM AUTHOR]

An effective method was developed for the preparation and x-ray diffraction analysis of the spatial structure of 7-hydroxy-5-oxo-2,3-dihydro-5 H-[1, 3]thiazolo[3,2- a]pyrimidine-6-carboxylic acid ethyl ester, which is of interest as a starting material for the synthesis of new, potentially biologically active derivatives of thiazolo[3,2- a]pyrimidine hydrogenated in the thiazole part of the molecule. [ABSTRACT FROM AUTHOR]

Aseries of 5-(heterylmethylene)hexahydropyrimidin-2,4,6-triones was synthesized and their activities against Staphylococcus aureus, Bacillus subtilis, and Escherichia coli were assessed, with determination of minimum inhibitory concentrations. [ABSTRACT FROM AUTHOR]

Azeolite ZSM-5 catalyzed simple, one-pot solvent-free, cost-effective and environmental benign protocol for the synthesis of dihydropyrimidines (DHPMs) have been developed. Aseries of substituted 1,4-DHPM derivatives have been synthesized by one-pot Biginelli type cyclocondensation of ethylacetoacetate, aromatic/heteroaromatic aldehydes, and urea/thiourea with a catalytic amount of zeolite under solvent-free protocol in a sufficiently high yield. The catalyst is recyclable and can be used repeatedly. [ABSTRACT FROM AUTHOR]

Several N-acyl phenothiazine chalcones were prepared by the condensation of various aldehydes with N-acyl phenothiazine in alcoholic KOH. The chalcones were further treated with urea and thiourea to obtain 6-(substituted phenyl)-4-(10H-phenothiazin-10-yl)pyrimidin-2(1H)-ones/thiones. All the synthesized compounds were screened for their antimicrobial activity and characterized by elemental analyses, IR, H NMR, and mass spectroscopy. [ABSTRACT FROM AUTHOR]

Three-component condensation of thiourea, ethyl acetoacetic ester, and anisaldehyde was performed to synthesize ethyl-4-(4-methoxyphenyl)-6-methyl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate. This compound interacted with aromatic aldehydes to yield the corresponding styryl derivatives. The hypotensive activity of the compounds synthesized here was assessed. [ABSTRACT FROM AUTHOR]

A series of new 2-substituted 8-methyl-5-(2-pyridinylethyl)-2,3,4,5-tetrahydro-1 H-pyrido[4,3- b]indoles have been synthesized. Their activity profiles were studied on a broad panel of therapeutic targets including GPC-receptors, ion channels, and neurotransmitter transporters. One of the studied compounds, 2-methyl-3-{2-[8-methyl-5-(2-pyridin-2-ylethyl)-2,3,4,5-tetrahydropyridino[4,3- b]indol-2-yl]ethyl}-6,7,8,9-tetrahydropyrido[1,2- a]pyrimidin-4-one, was found to be a highly active antagonist of adrenergic α, α, α, and α receptors and serotonin 5-HT, 5-HT, 5-HT, and 5-HT receptors. The results were considered in terms of structure-activity relationships. It was established that introduction of bulky substituents into the 2-position of the other synthesized 8-methyl-5-(2-pyridinylethyl)-2,3,4,5-tetrahydro-1 H-pyrido[4,3- b]indoles led to an activity decrease of the corresponding derivatives as compared with that of the 2,8-dimethyl analogs. [ABSTRACT FROM AUTHOR]

New 3-(arylsulfonyl)-2-(methylthio)pyrazolo[1,5- a]pyrimidines with a substituent amino group in the 7 position were synthesized and their 5-HT antagonist activity was studied. The transition from 7-amino and 7-dimethylamino derivatives to 7-aminoalkyl derivatives was found to lead to a significant decrease in activity; a similar pattern was seen on substitution of the methyl group in position 5 by a phenyl or thiophen-2-yl substituent. The most active (at the picomolar level) compounds were 5-methyl-2-(methylthio)-3-(phenylsulfonyl) pyrazolo[1,5- a]pyrimidin-7-amine and N, N,5,6-tetramethyl-2-(methylthio)-3-(phenylsulfonyl)pyrazolo-[1,5- a]pyrimidin-7-amine ( K = 700 pM). The first member of the hydrogenated pyrazolo[1,5- a]pteridine class -5,6,9-trimethyl-2-(methylthio)-3-(phenylsulfonyl)-6,7,8,9-tetrahydropyrazolo[1,5- a]pteridine ( K = 14.4 nM) was synthesized. These relationships between structure and 5-HT antagonist activity support the adequacy of our pharmacophore model, such that it can be used for the further search for new highly effective 5-HT antagonists. [ABSTRACT FROM AUTHOR]

Reactions of 4,6-dihydrazino-5-nitro- and 2-methylthio-4-hydrazino-6-chloro-5-( p-alkoxybenzyl)pyrimidines with carbonyl compounds and aryl- and cyclohexylisothiocyanates were studied. The influence of the products on DNA methylation and their in vitro antitumor properties were studied. [ABSTRACT FROM AUTHOR]

3-(Arylsulfonyl)-2-(methylthio)pyrazolo[1,5- a]pyrimidines containing substituents with an amine in the 6-position were synthesized. Their structure-activity (antagonist) relationship was studied with respect to serotonin 5-HT receptors. It was shown that 2-(methylthio)-3-(phenylsulfonyl)- and 2-(methylthio)-3-(3-chlorophenylsulfonyl)pyrazolo[1,5- a]pyrimidin-6-amines, the activity of which was comparable with 3-(arylsulfonyl)-2-(methylamino)pyrazolo[1,5- a]pyrimidin-6-amines and 3-(arylsulfonyl)-2-(methylamino)-and 3-(arylsulfonyl)-2-(methylthio)pyrazolo[1,5- a]pyrimidin-7-amines that were reported earlier, were the most active picomolar ligands. [ABSTRACT FROM AUTHOR]

The synthesis of sydnone sulfonamides bearing thiazole, benzothiazole and pyrimidine heterocycles is described. The newly synthesized compounds were characterized by IR, NMR and elemental analysis and evaluated for their antibacterial activity against some important Gram-positive and Gram-negative bacterial strains. Most of these compounds showed good to moderate activity against tested microbes. [ABSTRACT FROM AUTHOR]

New 2-S-4,5,6-substituted pyrimidines have been prepared via the reaction of 2-mercaptopyrimidines with allyl-, methallyl-, and substituted-benzyl chlorides, chloroacetamide, and chloracetic, á-bromopropionic, and á-bromocaproic acids. Reactions of 2-methylthio-derivatives with morpholine, piperidine, and o- and p-anisidines yielded the corresponding 2-amino-derivatives. The antitumor properties of the synthesized compounds have been studied. [ABSTRACT FROM AUTHOR]

Novel bioactive 2-phenyl-3-(4,6-diarylpyrimidin-2-yl)thiazolidin-4-ones 12-22 were synthesized with good yields in a short reaction time by the 'one-pot' multicomponent reaction of the appropriate 2-amino-4,6diarylpyrimidines, benzaldehyde and thioglycolic acid under microwave irradiation in the presence of an activated fly ash catalyst in dry medium. The characterization of these compounds was confirmed by melting point, elemental analysis, mass spectrometry, FT-IR spectroscopy, and one-dimensional NMR (H and C) spectroscopic data. In search for new leads toward potent antimicrobial agents, all the synthesized compounds have been tested in vitro for their antibacterial activity against Bacillus subtilis and Micrococcus luteus and antifungal activity against Aspergillus niger, Candida albicans, Candida 6 and Candida 51, and the results are discussed. [ABSTRACT FROM AUTHOR]

The effect of tautomerism on the structure of products from the reaction of N-(6-methyl-2,4-dioxo-1,2,3,4-tetrahydro-5 H-pyrimidinesulfone)- N′-isonicotinoylhydrazide (kristafon) with acids (hydrochloric, phosphoric, acetic, oxalic, succinic, citric, hyaluronic) and bases [sodium hydroxide, triethanolamine, tris-(hydroxymethyl)aminomethane] in aqueous media has been studied using UV, IR, PMR, and C NMR spectroscopy techniques. The properties of kristafon are compared to those of analogous compounds containing pyridine (isonicotine hydrazide, sulfotolylisonicotine hydrazide) and pyrimidine [ bis- p-(2,4-dioxo-6-methylpyrimidinyl-5-sulfonamino)-diphenylsulfone] fragments in acid-base media. It is shown that the immunotropic activity of kristafon phosphate and kristafon are improved in hyaluronic acid solution. [ABSTRACT FROM AUTHOR]

The reactions of 6-acyl-7-aryl-4,7-dihydrotetrazolo [1,5-a]pyrimidin-5-carboxylates with hydrazine hydrate were used to synthesize 8-methyl-9-aryl-and 8,9-diaryl-4,9-dihydrotetrazolo [1',5':1,2]pyrimidino[4,5-d]pyrazin-5-ones (I – XXX). Compounds I – XXX were found to have moderate antimicrobial activity. [ABSTRACT FROM AUTHOR]

A series of 4-[4-(2, 4-dichloro-5-fluorophenyl)-6-(4-methoxyphenyl)pyrimidine-2-yl]-1-(arylaminocarbonyl/thiocarbonyl)semicarbazides was synthesized and their in vitro antibacterial activity was studied. [ABSTRACT FROM AUTHOR]

A series of pyrimidinophanes containing two uracil units and nitrogen atoms in bridging polymethylene chains –(CH2) nN(Et)(CH2) m– ( n, m = 5, 6) have been synthesized. The uracil moieties are represented by 6-methyl-, 5-decyl-6-methyl-, and 5-fluorouracils. Quaternization of the bridging N atom with ethylbromide or n-decylbromide yielded amphiphilic pyrimidinophanes, which were evaluated for their antibacterial and antifungal activity in terms of minimal inhibiting concentration (MIC) against Gram-positive and Gram-negative bacteria and fungi. It has been found that MICs of the amphiphilic pyrimidinophanes decrease with increasing lipophilicity of the alkyl substituents at the bridging N atoms and with increasing polymethylene N(pyr)–N chain length (in some cases MIC against Staphylococcus aureus is below 1 ìg/mL). The MICs increase dramatically upon introduction of lipophilic n-decyl substituents at C(5) atoms of the uracil moiety. The results can be used in the search for new highly effective antimicrobial agents. [ABSTRACT FROM AUTHOR]

Methods for the synthesis of new heterosystems including condensed pyrano[4′,3′:4,5]pyrido[2,3- b]-thieno[3,2- d]thiazolo(thiazino, thiazepino)[3,2- a]pyrimidines, thiazolo(thiazino, thiazepino)[3″,2″:1′,2′]pyrimido[4′,5′:4,5]thieno[2,3- c]isoquinolines, and cyclopenta[4′,3′:4,5]pyrido[2,3- b]thieno[3,2- d]thiazolo(thiazino)[3,2- a]pyrimidines are developed. The synthesis is carried out on the basis of 1-amino-2-ethoxycarbonylpyrano[4,3- d]thieno[2,3- b]pyridines and -thieno[2,3- b]isoquinolines. Antitumor and anticonvulsant properties of the synthesized products have been evaluated. Compounds possessing low toxicity and moderate biological activity are found. [ABSTRACT FROM AUTHOR]

Derivatives of dipyrimido[4,5-b][5,4-f]-1,4-thiazepine were synthesized and some of their properties were studied. [ABSTRACT FROM AUTHOR]

Methods for the synthesis of condensed thieno[3,2-d]pyrimidines based on pyrano[4,3-d]thieno[2,3-b]pyridines and thieno[2,3-b]isoquinolines have been developed and a series of new derivatives have been synthesized. The anticonvulsant activity of the synthesized compounds has been studied. Several compounds possessing specific anticonvulsant activity with respect to corazole-induced convulsions are revealed. [ABSTRACT FROM AUTHOR]

A series of thio-5-nitropyrimidine (thio-5-NP) derivatives was synthesized using the reactions of chlorine-substituted 5-NPs with various aromatic and boron-containing thiols. Reactions of 4,6-dithio-5-NP derivatives with nucleophiles were studied. Stable 2-σ-adducts were obtained using a boron-containing 4,6-dithio-5-NP derivative. The interaction of an aromatic sulfide of 5-NP with 1-phenyl-3-methylpyrazol-5-one led to substitution at one of the arylthio groups. The NMR and mass spectra of the synthesized compounds were obtained; the 2-oxy-σ-adduct was characterized by x-ray diffraction. [ABSTRACT FROM AUTHOR]

Pyrimidine derivatives are widely used for the treatment of viral diseases and cancer. The analysis of pyrimidine derivatives is typically performed using various chromatographic techniques, in particular, reversed-phase high performance liquid chromatography (HPLC). The separation is typically carried out with (7–30)-cm-long C8 and C18 silica gel columns, mainly at room temperature, and a 1–1.5 ml-min eluent flow rate. The column is eluted in an isocratic or gradient system, and a variety of mobile phases have been proposed. The detection is based on optical absorption or fluorescence measurements, or makes use of mass spectrometry. Various methods of extraction of pyrimidine derivatives from biological samples are discussed, and the corresponding detection limits are presented. [ABSTRACT FROM AUTHOR]

Optimum conditions for the spectrophotometric determination of pyrimidine derivatives in biological fluids of humans are determined. This method has been used for the investigation of the pharmacokinetics of the new immunomodulant ximedone in humans, dogs, and rats upon administration of the drug in different ways. Interspecific relationships of the key parameters of ximedone pharmacokinetics are established. [ABSTRACT FROM AUTHOR]

A series of new 2-S-substituted pyrimidine derivatives has been synthesized via the interaction of 2-mercaptopyrimidines with various alkylbromides, chloracetamide, and unsubstituted and substituted benzyl chlorides. The synthesized compounds have been tested with respect to antitumor activity. [ABSTRACT FROM AUTHOR]

A series of 1,3-bis(5-ammoniopentyl)-6-methyluracil dihalides with the anticholinesterase type of activity have been synthesized and characterized with respect to toxicity and myorelaxant activity. The obtained compounds exhibit high toxicity with respect to mice and belong to the class of low/practically zero toxicity with respect to daphnia. Under conditions of functional loading (treadmill running test) in mice, the compounds with small-volume electron-acceptor substitutes (F, NO2, CN, CH2 OCH3, C(O)OCH3 etc.) at the quaternary nitrogen atoms in the benzyl radical are more effective (upon intraperitoneal injection) and safer than the reference drugs (proserine and BW284c51) and induce the development of a clearly pronounced myorelaxant effect with a duration of no less than 1 day with ED50 = 0.04 – 0.09 µ-M/kg and LD50/ED50 up to 56.25. [ABSTRACT FROM AUTHOR]

The article cites a study which focused on the synthesis and pharmacological activity of &b.omega;-(4-phenylpiperazin-1-yl) alkylthiopyrimidines. The researchers synthesized and characterized a series of N-phenylpiperazine derivatives containing a mercaptopyrimidine cycle, which plays the role of a fragment favoring an increase in the affinity of compounds to adrenoreceptors of blood vessels. The synthesized &b.omega;-(4-phenylpiperazin-1-yl) alkylthiopyrimidines possess hypotensive activity, which can be related to their interaction with alpha adrenoreceptors of peripheral blood vessels.

Focuses on the synthesis and biological activity of alpha,omega-bis(ammonio)alkalis containing oxopyrimidinyl radicals. Yields and physicohemical characteristics of the synthesized compounds; Infrared absorption spectra; Data on the toxicity, myorelaxant activity and related therapeutic breadth of compounds.

Summarizes data on the synthesis and chemical properties of natural uracils. Methods used for the synthesis of uracils, namely condensation of urea or thiourea with carbonyl compounds and synthesis of substituted pyrimidines; Representation of carbonyl compounds by the derivatives of acetic, propionic, malonic, and succinic acids.

We report the development of methods for the preparation of new heterosystems - condensed pyrano[4″,3″:4′,5′]pyrido[3′,2′:4,5]thieno[2,3- e][1,2,4]triazolo[4,3- c]pyrimidines, [1,2,4]triazolo[3″,4″:6′,1']pyrimido[4',5':4,5]thieno[2,3]isoquinolones, and cyclopenta[4',5']pyrido[3',2':4,5]thieno[2,3- e][1,2,4]triazolo [4,3- c]pyrimidines. The anticonvulsive activity of these compounds was studied. [ABSTRACT FROM AUTHOR]

A new synthesis of 2-substituted-4H-chromen-4-ones (IVa-c) and 4-(2-hydroxyphenyl)-6-substituted pyrimidin-2(5H)-one/thiones (Va - Vc)/(VIa - VIc) derivatives is reported. First, benzoyloxy esters are converted into their 1,3-diones (IIIa - IIIc) by using dry KOH in pyridine via the Baker - Venkataraman transformation reaction. Then, 1,3-diones thus obtained are cyclised into 2-substituted-4H-chromen-4-ones (IVa - IVc) and 4-(2-hydroxyphenyl)-6-substituted pyrimidin-2(5H)-one/thiones (Va - Vc)/(VIa - VIc) by refluxing in acetic acid and urea/thiourea in ethanol, respectively. The newly synthesized compounds were characterized by IR, H NMR, and mass spectroscopy and elemental analysis and tested for their antibacterial and antifungal activity. [ABSTRACT FROM AUTHOR]

eries of novel triazole fused tetracyclic thienopyrimidines ( III - X) were synthesized from the corresponding precursor 5-amino-4-cyano-3-methylthiophene-2-carboxylic acid ethyl ester I. The precursor were in turn prepared via the Gewald reaction. Structures of all the newly synthesized compounds were characterized by spectral and analytical data. All the tested compounds displayed promising antibacterial and antifungal activities. [ABSTRACT FROM AUTHOR]

Methods for the synthesis of condensed thieno[3,2- d]pyrimidines based on 3,3-dimethyl-8-morpholino-6thioxo-3,4,6,7-tetrahydro-1H-pyrano[3,4- c]pyridine-5-yl cyanide have been developed. The neurotropic properties of the synthesized compounds have been investigated. Compounds possessing anticonvulsant activity and sedative properties are found. These compounds also exhibit an activating effect that makes them analogous to the well-known drug diazepam. [ABSTRACT FROM AUTHOR]

The compounds N-(4-propoxybenzenesulfonyl)- N′-(4-methoxybenzyl)urea and 2- p-toluenesulfonamido-4,6-dihydroxy-5-(3-carbomethoxy-4-propoxybenzyl)pyrimidine have been synthesized. It is established that these compounds possess pronounced hypoglycemic activity. [ABSTRACT FROM AUTHOR]

Eighteen methyl-7-aryl(heteryl)-6-(2-thienoyl)-4,7-dihydrotetrazolo[1,5- a]pyrimidine-5-carboxylates (I – XVIII) have been synthesized via the interaction of methyl esters of acylpyruvic acids with a mixture of aromatic or heterocyclic aldehydes and 5-aminotetrazole monohydrate. The proposed structures of the synthesized compounds were confirmed by IR spectroscopy and PMR spectrometry. Several compounds have been tested for antimicrobial activity. [ABSTRACT FROM AUTHOR]

A series of condensed heterocycles containing the pyrazolo[1,5- a]pyrimidine moiety were synthesized from 5-amino-3-methyl-4-phenylpyrazole. The spectra of potential biological activity of the synthesized compounds were determined using computer-aided prediction methods, which showed that the most probable properties were corticotropin-releasing hormone antagonism, cyclooxygenase inhibition, and neuroleptic, nootropic, and cardioprotector activity [ABSTRACT FROM AUTHOR]

Reactions of 2-methylthio-4,6-dichloro-5-(4-alkoxybenzyl)pyrimidines with aliphatic and aromatic primary and secondary amines and sodium methoxide were used to synthesize the corresponding 4-amino-and 4-methoxy-6-chloropyrimidines. The antitumor properties of the synthesized compounds have been studied. [ABSTRACT FROM AUTHOR]

New methods for the synthesis of 4-substituted 6,7-dihydro-7,7-dimethyl-5-oxo-9H-pyrano-[4′,3′: 4,5]-thieno[3,2-e]imidazo[1,2-a]pyrimidines and their hydrochlorides are developed. The anticonvulsant and tranquilizer properties of newly synthesized compounds have been studied. [ABSTRACT FROM AUTHOR]

A series of thiuronium salts have been synthesized via reactions of various thioamides with 2-bromo-7-methyl-5-oxo-5H-1,3,4-thiazolo[3,2-a]pyrimidine. The products have been characterized with respect to antimicrobial activity. [ABSTRACT FROM AUTHOR]

A series of 1-aryl-4-(3′,4′,5′-trimethoxybenzoyl)piperazines (IIa - IIg) having structures containing 3,4,5-trimethoxybenzoyl fragments were synthesized and characterized. Compounds IIa and IIc - IIg demonstrated weak anxiolytic properties and moderately decreased the spontaneous motor activity in rats. Compound IIb exhibited anxiolytic activity comparable with that of buspirone but, in contrast to this reference drug, increased the motor activity of test animals. [ABSTRACT FROM AUTHOR]

The article cites a study which focused on the synthesis of cyano derivatives of pyrimidine bases and their effect on blood leukocyte system. The researchers synthesized cyanocytosine, cyanouracil, and cyanothymine and studied their influence on the blood leukocyte system in comparison to the effects of nonmodified pyrimidine bases. It was established that the treatments with cyanocytosine, cyanouracil, and cyanothymine lead to an increase in the total leukocyte count in peripheral blood. In the case of cyanocytosine, this effect is related to an increase in the number of lymphocytes, segmented neutrophils, and eosinophils.