Synthesis of 2,3,6-trideoxy sugar triazole hybrids as potential new broad spectrum antimicrobial agents.
Eur J Med Chem
; 83: 474-89, 2014 Aug 18.
Article
em En
| MEDLINE
| ID: mdl-24992075
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 µg/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 µg/mL against Staphylococcus aureus and Klebsiella pneumoniae and 3.12 µg/mL against methicillin- and vancomycin-resistant S. aureus. Compound 26 was the most potent anti-fungal candidate with MIC 0.39 µg/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.
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Base de dados:
MEDLINE
Assunto principal:
Triazóis
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Carboidratos
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Desenho de Fármacos
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Anti-Infecciosos
Idioma:
En
Ano de publicação:
2014
Tipo de documento:
Article