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

ÖZDEMİR A., Turan-Zitouni G., KAPLANCIKLI Z. A., Chevallet P.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.22, no.4, pp.511-516, 2007 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 22 Issue: 4
  • Publication Date: 2007
  • Doi Number: 10.1080/14756360601178424
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.511-516
  • Keywords: 4-arylidenamino-4H-1,2,4-triazole-3-thiol, mycobacterium, tuberculosis, antimycobacterials, TUBERCULOSIS
  • Bilecik Şeyh Edebali University Affiliated: No

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 H(37)Rv ( ATCC 27294), using the BACTEC 460 radiometric system and BACTEC 12B medium. Compound 2k showed an intereting activity at 6.25 mu g/mL with a 87 percentage inhibition.