Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 83, Issue -, Pages 474-489Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.06.048
Keywords
2,3,6-Trideoxy sugars; 1,2,3-Triazole; Molecular hybridization; Click chemistry; Antimicrobial agents; Penicillin binding protein
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Funding
- Council of Scientific and Industrial Research (CSIR), New Delhi, India
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Here, we describe a molecular hybridization inspired design and synthesis of novel 6-triazolyl 2,3,6-trideoxy sugars as promising new broad-spectrum antimicrobial agents using click chemistry in key step. These compounds showed MIC between 0.39 and 50 mu g/mL against different native and resistant bacteria and fungi with no toxicity. Among them, compound 29 was the most active molecule with MIC 0.78 mu g/mL against Staphylococcus aureus and Klebsiella pneumoniae and 3.12 mu g/mL against methicillin- and vancomycin-resistant S. aureus. Compound 26 was the most potent anti-fungal candidate with MIC 0.39 mu g/mL against Trichophyton mentagrophytes. Compound 46 was found to be promising with broad-spectrum activity against both bacterial and fungal strains. The bioinformatic studies involving bacteria's protein co-crystals prompted penicillin binding protein-2 as the most likely target of these compounds. (C) 2014 Elsevier Masson SAS. All rights reserved.
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