Synthesis of some 4-arylidenamino-4H-1,2,4-triazole-3-thiols and their antituberculosis activity.
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 triazoles were synthesized and evaluated for antituberculosis activity. A series of 4-arylidenamino-4H-1,2,4-triazole-3-thiol derivatives (2a-n) were synthesized from the treatment of 4-amino-4H-1,2,4-triazoles-3-thiol (1) with the respective aldehydes and were evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294), using the BACTEC 460 radiometric system and BACTEC 12B medium. Compound 2k showed an intereting activity at 6.25 microg/mL with a 87 percentage inhibition.
Ozdemir
Ahmet
A
Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, 26470 Eskisehir, Turkey. ahmeto@anadolu.edu.tr
Turan-Zitouni
Gulhan
G
Kaplancikli
Zafer Asim
ZA
Chevallet
Pierre
P
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000494:pharmacology*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests / Q000379:methods; D008956:Models, Chemical; D009169:Mycobacterium tuberculosis / Q000378:metabolism*; D013055:Spectrophotometry, Infrared; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D014230:Triazoles / Q000737:chemistry / Q000494:pharmacology*; D014376:Tuberculosis / Q000188:drug therapy*
D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D013438:Sulfhydryl Compounds; D014230:Triazoles