Studies on the synthesis and antibacterial activity of 3,6-disubstituted 1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles

Eur J Med Chem. 2012 Jan;47(1):580-4. doi: 10.1016/j.ejmech.2011.10.055. Epub 2011 Nov 6.

Abstract

Treating infections caused by drug-resistant bacterial strains constitutes one of the most essential challenges for medicine nowadays. A range of new derivatives of 1,2,4-triazolo[3,4-b]1,3,4-thiadiazole have been synthesized and evaluated for their in vitro antimicrobial activity. Compounds 1-8 indicated high activity towards Gram-positive bacteria, which was up to 16 times more than currently used antibiotics. To the best of our knowledge, the derivatives obtained by us are the most active among the 3-aryl-6-arylamino-1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles known until now.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship
  • Thiadiazoles / chemical synthesis*
  • Thiadiazoles / chemistry
  • Thiadiazoles / pharmacology*

Substances

  • Anti-Bacterial Agents
  • Thiadiazoles