Synthesis and antituberculosis activity of new 3-alkylsulfanyl-1,2,4-triazole derivatives

Kaplancikli Z., Turan-Zitouni G., Chevallet P.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.20, no.2, pp.179-182, 2005 (SCI-Expanded) identifier identifier identifier


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 BACTEC12B medium and results were screened in-vitro, using BACTEC 460 Radiometric System against Mycobacterium tuberculosis H(37)Rv ( ATCC 27294) at 6.25 mu g/ml and the tested compounds showed considerable inhibition ranging from 58 - 84%.