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|Title:||Synthesis of 2,3,6-trideoxy sugar triazole hybrids as potential new broad spectrum antimicrobial agents|
Mishra, N N
Shukla, P K
Prabhakar, Y S
Shaw, A K
|Keywords:||2,3,6-Trideoxy Sugars;1,2,3-Triazole;Molecular Hybridization;Click Chemistry;Antimicrobial Agents;Penicillin binding protein|
|Description:||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 0.39-50µg/mL against different native and resistant bacteria and fungi with no toxicity. Among them, compound 29 was the most active molecule with MIC 0.78µg/mL against Staphylococcus aureus and Klebsiella pneumoniae and 3.12µg/mL against methicillin- and vancomycin-resistant S. aureus. Compound 26 was the most potent anti-fungal candidate with MIC 0.39µg/mL against T. 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.|
|Other Identifiers:||European Journal of Medicinal Chemistry, 2014, 83, 474-89|
|Appears in Collections:||Medicinal and Process Chemistry|
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