Synthesis and pharmacological activities of some new 3-substituted-4-amino-5-mercapto-1,2,4-triazoles.

Abstract

In this study, various 3-β-[(N-benzenesulphonyl/tosyl)-4-(un) substituted anilino]ethyl-4-amino-5-mercapto-4(H)-1,2,4-triazoles (5a–f), with biologically active ‘sulphonamide’ moiety as the side chain have been prepared. The structures of the newly synthesised compounds have been established on the basis of their spectral data and elemental analysis. All the compounds were evaluated for antimicrobial activities against Escherichia coli, Bacillus cirroflagellosus, Aspergillus niger and Colletotrichum capsici. Most of the compounds investigated exhibited significant antifungal activity against Colletotrichum capsici, even greater than fluconazole, the standard used. Only two compounds 3f (59%) and 5e (67%), have shown moderate antituberculosis activity. All the triazoles exhibited moderate degree of antiinflammatory activity and least ulcerogenecity. Most of the compounds have shown significant analgesic activity (81.02–120.72%) in comparison with aspirin (49.39%). In the MES method, only compound 3e exhibited a protection of 66.66%, whereas others exhibited minimum protection of (33.33%).