A series of 2-(1H-indol-2-yl)-3-acrylonitrile derivatives, 2a–x, 3, 4a–b, 5a–d, 6a–b, and 7, were synthesized as potential antitumor antimicrobial agents. The structures the prepared compounds evaluated based on elemental analysis, IR, 1H- 13NMR, well MS spectra. X-ray crystal analysis representative 2l showed that acrylonitrile double bond was Z-configured. All screened at National Cancer Inst...

The aim of the work. 1,2,4-triazole derivatives possess a wide range pharmacological activity, so they are used for development drugs and active pharmaceutical ingredients. Due to reactivity 1,2,4-triazoles there many options their further structural modification on different reaction centers. Therefore, work was obtain new S-substituted 1,2,4-triazole-3-thiols, study physicochemical parameters...

The synthesis of series of tripodal ligands: N,N-bis((3-carboxyethyl-5-dimethyl-1H-pyrazol-1yl)methyl)phenylamine L1, N,N-bis((3,5-dimethyl-1H-pyrazol-1-yl)methyl)phenylamine L2, N,N-bis((3carboxyethyl-5-dimethyl-1H-pyrazol-1-yl)methyl)pyridin-2-ylamine L3, N,N-bis((3,5-dimethyl-1H-pyrazol1-yl)methyl)pyridin-2-amine L4, N,N-bis((3-carboxyethyl-5-dimethyl-1H-pyrazol-1-yl)methyl)-2nitrophenylamin...

Purpose: The article is aimed to synthesize,characterize and screening the biological activity of a series of Synthesis of 1-(2-(3-(3-chloro-1-(4-substituted phenyl)-4-tetrazole-2-yl)-1H-indol-1-yl)acetyl)-4-(2-(4substituted phenyl)hydrazono)-3-(trifluoromethyl)-1H-pyrazol-5(4H)-one 4(a-f). Indole-3-carbaldehyde and chloro ethyl acetate were dissolved in DMF. To this reaction mixture anhydrous ...

Reactions of hydrazonoyl halides and each of methyl 2-(1-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)ethylidene)hydrazine-1-carbodithioate and 2-(1-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)ethylidene)hydrazine-1-carbothioamide afforded 2-(1-(5-methyl-1-phenyl-1H-1,2,3-triazol-4-yl)ethylidene)hydrazono)-3-phenyl-5-substituted-2,3-dihydro-1,3,4-thiadiazoles and 5-(4-substituted)diazenyl)-2-(2-(1-(5-...

2-(3-(1H-Indol-3-yl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazol-1-yl)-4-substituted-5-(substituted diazenyl)thiazoles and 2-(1H-indol-3-yl)-9-substituted-4,7-disubstituted pyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrimidin-5(7H)-ones were synthesized via reaction of hydrazonoyl halides with each of 3-(1H-indol-2-yl)-5-(p-tolyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide and 7-(1H-indol-3-yl)-2- thioxo-5-substi...

A small series of indol-3-yl-oxoacetamides was synthesized starting from the literature known N-(adamantan-1-yl)-2-(5-(furan-2-yl)-1-pentyl-1H-indol-3-yl)-2-oxoacetamide (5) by substituting the 1-pentyl-1H-indole subunit. Our preliminary biological evaluation showed that the fluorinated derivative 8 is a potent and selective CB₂ ligand with Ki = 6.2 nM.

Benzimidazole is one of the most important heterocyclic groups manifesting various biological properties, such as antibacterial, antifungal, antimicrobial, antiprotozoal and antihelmintic activities. Several benzimidazole derivatives are also active as inhibitors of type I DNA topoisomerases. In this study, three 1H-benzimidazole derivatives with different electronic characteristics at position...

We have developed a liquid-phase route for combinatorial synthesis of novel substituted 5-(1,2,4-oxadiazol-5-yl)-3,4-dihydropyrimidine-2(1H)-thiones. Biginelli-type three-component condensation of 1-(3-aryl-1,2,4-oxadiazol-5-yl)acetones, thiourea, and benzaldehydes is shown to result in new 5-(1,2,4-oxadiazol-5-yl)-3,4-dihydropyrimidine-2(1H)-thione heterocyclic system. If salicylaldehydes are ...