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

ABSTRACT

To 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. The compounds were characterised by elemental analysis, IR, [1]H 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. The 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. All the title compounds showed good antibacterial and antifungal activities. Virtual screening studies reveal that the compounds under study possess excellent drug-like characteristics