D. N. Rao, A. Prasad, Y. N. Spoorthy
Dec 1, 2014
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0
Influential Citations
7
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Journal
Journal of Taibah University Medical Sciences
Abstract
Abstract Objectives 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. Methods 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. Results 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. Conclusion All the title compounds showed good antibacterial and antifungal activities. Virtual screening studies reveal that the compounds under study possess excellent drug-like characteristics.