Synthesis of some 4-arylidenamino-4H-1,2,4-triazole-3-thiols and their antituberculosis activity

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 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 μg/mL with a 87 percentage inhibition.

Keywords::

• 4-Arylidenamino-4H-1,2,4-triazole-3-thiol
• mycobacterium
• tuberculosis
• antimycobacterials

Acknowledgements

The Authors are thankful to the Tuberculosis Antimicrobial Acquisition & Coordinating Facility (TAACF) in the USA for the in vitro evaluation of antimycobacterial activity.