Synthesis, characterization and pharmacological studies of sulphur containing 1,2,4-triazole derivatives
| Autor: | L.K. Ravindranath, D.V. Narayana Rao, Yadati Narasimha Spoorthy, D. Raghunatha Rao, A. Raghavendra Guru Prasad |
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| Rok vydání: | 2014 |
| Předmět: |
مشتقات ٤
٢ ١-الترايازول biology نشاط مضادات الميكروبات In silico خصائص شبه دوائية Substituent 1 2 4-Triazole 1 2 4-triazole derivatives Biological activity Spectral analysis General Medicine Antimicrobial activity biology.organism_classification Antimicrobial Synthesis chemistry.chemical_compound Drug-like characteristics chemistry تصنيع Nitro Proton NMR Organic chemistry التحليل الطيفي Bacteria |
| Zdroj: | Journal of Taibah University Medical Sciences. 9:293-300 |
| ISSN: | 1658-3612 |
| DOI: | 10.1016/j.jtumed.2014.06.002 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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