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

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.

Two new derivatives (5 and 6) are as effective towards the MRSA strain as vancomycin.Figure optionsDownload as PowerPoint slideHighlights
► 3,6-Disubstituted-1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles have been synthesized.
► Antibacterial activities were up to 16-fold higher as compared to reference drugs.
► Molecular target is still unknown.