Synthesis and evaluation of novel benzene-ethanol bearing 1,2,4-triazole derivatives as potential antimicrobial agents

The azole pharmacophore is still regarded as a viable lead structure for the synthesis of more efficacious and broad-spectrum antimicrobial agents. In this study, a novel series of triazole derivates that are structurally related to the famous antimicrobial azole pharmacophore were synthesized and t...

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Veröffentlicht in:Medicinal chemistry research 2017, Vol.26 (1), p.44-51
Hauptverfasser: Li, Bochao, Zhang, Dawei, Zhang, Yumin, Dan Jiang, Li, Shuang, Lei, Wei, Wang, Huiying, Lin, Feng
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Sprache:eng
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Zusammenfassung:The azole pharmacophore is still regarded as a viable lead structure for the synthesis of more efficacious and broad-spectrum antimicrobial agents. In this study, a novel series of triazole derivates that are structurally related to the famous antimicrobial azole pharmacophore were synthesized and the structures of them were characterized by spectral (IR, 1 H NMR, 13 C NMR, and MS spectra) analysis. Antimicrobial activity was measured against both bacteria and fungus. In vitro antimicrobial evaluation showed that five compounds had growth inhibitory effects on the tested Gram-positive bacteria and fungus with special efficacy. Potential antibacterial and antifungal activities are incorporated in these triazole compounds. Results of antimicrobial activities also revealed that compounds ( 5a–i ) were the potent antibacterial and antifungal agents as compared to standard drugs (ciprofloxacin and itraconazole), and thus could be promising new lead molecules.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-016-1724-6