Synthesis and bioactivity of a novel series of 3,6-disubstituted 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles

A novel series of 3,6-disubstituted 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazoles were synthesized by the condensation of 4-amino-5-[2-(4-chlorophenoxymethylbenzimidazole)-1-methylene]-3-mercapto-1,2,4-triazole with various (un)substituted aromatic acids in the presence of phosphorous oxychloride. These compounds were investigated for their inhibitory activity to E. coli methionine aminopeptidase (EcMetAP1). Some of the tested compounds showed significant inhibitory activity.