title: Synthesis and antituberculosis activity of new 3-alkylsulfanyl-1,2,4-triazole derivatives.
abstract: The increasing clinical importance of drug-resistant mycobacterial pathogens has lent additional urgency to microbiological research and new antimycobacterial compound development. For this purpose, new alkylsulfanyltriazoles were synthesized and evaluated for antituberculosis activity. The reaction of thienyl-2-acetic acid with thiocarbohydrazide gave the mercaptotriazoles (II). The 4-amino-5-(2-thienylmethyl)-3-[1-(2-thienyl)-3-aryl) propion-3-yl] sulfanyl-4H-1,2,4-triazole (III) derivatives were synthesized by reacting the mercaptotriazoles with chalcones (I). Antituberculosis activities of the synthesized compounds were determined by broth microdilution assay, the Microplate Alamar Blue Assay, in BACTEC 12B medium and results were screened in-vitro, using BACTEC 460 Radiometric System against Mycobacterium tuberculosis H37Rv (ATCC 27294) at 6.25 microg/ml and the tested compounds showed considerable inhibition ranging from 58-84%.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Anadolu University, Eskişehir 26470, Turkey. zakaplan@anadolu.edu.tr
authors.forename: Zafer Asim
authors.initials: ZA
authors.lastname: Kaplancikli
authors.forename: Gülhan
authors.initials: G
authors.lastname: Turan-Zitouni
authors.forename: Pierre
authors.initials: P
authors.lastname: Chevallet
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology; D000995:Antitubercular Agents / Q000494:pharmacology*; D047188:Chalcones / Q000737:chemistry; D003470:Culture Media / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D009169:Mycobacterium tuberculosis / Q000378:metabolism; D010078:Oxazines / Q000494:pharmacology; D013696:Temperature; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry; D014230:Triazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D014966:Xanthenes / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D047188:Chalcones; D003470:Culture Media; D010078:Oxazines; D013844:Thiazoles; D014230:Triazoles; D014966:Xanthenes; C005843:resazurin; C045575:1,2,4-triazole