CSIR Central

Synthesis of 2,3,6-trideoxy sugar triazole hybrids as potential new broad spectrum antimicrobial agents

IR@CDRI: CSIR-Central Drug Research Institute, Lucknow


Field	Value

Creator	Sharma, Smriti Saquib, Mohammad Verma, Saroj Mishra, N N Shukla, P K Srivastava, Ranjana Prabhakar, Y S Shaw, A K

Date	2014-09-29T10:34:07Z 2014-09-29T10:34:07Z 2014

Identifier	European Journal of Medicinal Chemistry, 2014, 83, 474-89 http://hdl.handle.net/123456789/1413

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.

Format	1334122 bytes application/pdf

Language	en

Relation	CSIR-CDRI Communication No. 8723

Subject	2,3,6-Trideoxy Sugars 1,2,3-Triazole Molecular Hybridization Click Chemistry Antimicrobial Agents Penicillin binding protein

Title	Synthesis of 2,3,6-trideoxy sugar triazole hybrids as potential new broad spectrum antimicrobial agents

Type	Article