Recent advances bioactive 1,2,4-triazole-3-thiones

Design, Synthesis, Characterization and Antimicrobial Evaluation of Some Heterocyclic Condensed Systems with Bridgehead Nitrogen from Thiazolotriazole Class

“…33) In order to obtain condensed heterocyclic compounds 3a-c, in a first stage, new intermediates S-alkylates 1,2,4-triazole 2a-c were synthesized by the reaction of triazoles 1a-c with 2-bromo-4′-fluoroacetophenone. 2-(4-(4-X-Phenylsulfonyl)phenyl)-6-(4-fluorophenyl)thiazolo [3,2-b] [1,2,4]triazoles 3a-c were synthesized from S-alkylated 1,2,4-triazoles 2a-c, by cyclization in sulfuric acid medium. [3,2-b] [1,2,4]triazol-6(5H)-one 4a-c were obtained by reaction of triazoles 1a-c with 4-fluorobenzaldehyde, chloroacetic acid and anhydrous sodium acetate, in the presence of acetic acid and acetic anhydride.…”

“…The fusion of triazole and thiazole rings can lead to thiazolotriazoles with superior biological properties due to mutual influence of the pharmacophores centers present in the molecule. Thus, literature data indicate that numerous thiazolo [3,2-b] [1,2,4] triazoles derivatives have been reported to possess antibacterial, [3][4][5][6][7][8][9] antifungal, 3,[6][7][8][9] anti-inflammatory, 3,10,11) analgesic, 3,10) antiproliferative, 12) anticonvulsant 13) properties. Also, thiazolo [3,2-b][1,2,4] triazol-ones have been studied for their properties with respect to their biological activities including anti-inflammatory, [14][15][16][17] analgesic, 15,17) anticancer, [18][19][20] antibacterial, 21) antifungal 21) and anticonvulsant.…”

“…Both triazole and thiazole rings are known that possess various biological properties, being present in composition of numerous drugs, especially with antimicrobial activity. 1,2) Among of the antimicrobial drugs are distinguished Itraconazole, Fluconazole, Voriconazole (drugs with 1,2,4-triazole ring), Sulfathiazole and Abafungin (drugs with thiazole ring). The fusion of triazole and thiazole rings can lead to thiazolotriazoles with superior biological properties due to mutual influence of the pharmacophores centers present in the molecule.…”

Synthesis and Evaluation of New Pyrazoline Derivatives as Potential Anticancer Agents

“…Recent studies have indicated that 1,3,4-oxadiazole derivatives exhibit potent anticancer activity against different cancer cell lines through the inhibition of different growth factors, enzymes and kinases including telomerase, histone deacetylase (HDAC), methionine aminopeptidase (MetAP), thymidylate synthase (TS), glycogen synthase kinase-3 (GSK), epidermal growth factor (EGF), vascular endothelial growth factor (VEGF), and focal adhesion kinase (FAK) [24][25][26]. Triazoles [27], tetrazoles [28], thiadiazoles [29], and pyrimidines [4] have also been reported to show anticancer activity.…”

Synthesis of Novel 4-R-1,2,4-Triazolin-5-Thiones Containing Space-Hindered Fragment of Phenol

“…Они проявляют противогрибковый (флуко-назол, интраконазол, вориконазол) [1], противо-воспалительный [2], седативный (триазолам, алфа-золам) [3], и противомикробный эффекты [4]. Среди меркапто-и тион-замещенных 1,2,4-триазо-лов было зарегистрировано большое число произ-водных, проявляющих антибактериальные [5,6], фунгицидные [7,8], противотуберкулензые [9] и антимикобактериальные [10] свойства, противора-ковую активность [11,12].…”