Synthesis, characterization and pharmacological studies of sulphur containing 1,2,4-triazole derivatives

ObjectivesTo design a five step procedure for the synthesis of seven novel sulphur containing 1,2,4-triazole derivatives namely 4-[(3-(4-Chloro-phenoxymethyl)-5-(4-substituted-benzylsulfonyl)-1,2,4-triazol-4-yl)methyl]-morpholine from 4-Chloro-phenol and Ethylbromoacetate as starting compounds and to screen for their pharmacological activity.MethodsThe compounds were characterised by elemental analysis, IR, 1H NMR and mass spectral data. All compounds were evaluated for antimicrobial activity against selected bacteria and fungi by the methods reported in the literature. The drug-like characteristics were assessed by in silico studies.ResultsThe compounds 8a, b and c showed moderate antimicrobial activity. Compounds 8d, e, f and g namely nitro, chloro, bromo and fluoro derivatives respectively, showed better antimicrobial activity than the other compounds. In silico studies indicated that the compound 8e with chloro substituent possesses excellent drug-like characteristics among the compounds under study.ConclusionAll the title compounds showed good antibacterial and antifungal activities. Virtual screening studies reveal that the compounds under study possess excellent drug-like characteristics.