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NH-1,2,3-Triazole-based Inhibitors of the VIM-2 Metallo-β-Lactamase: Synthesis and Structure-Activity Studies.

ABSTRACT: Metallo-ß-lactamases (MBL) are an emerging cause of bacterial resistance to antibiotic treatment. The VIM-2 ß-lactamase is the most commonly encountered MBL in clinical isolates worldwide. Described here are potent and selective small molecule inhibitors of VIM-2 containing the arylsulfonyl-NH-1,2,3-triazole chemotype that potentiate the efficacy of the ß-lactam, imipenem, in E. coli.

SUBMITTER: Weide T

PROVIDER: S-EPMC2901175 | biostudies-literature | 2010 Jul

REPOSITORIES: biostudies-literature

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NH-1,2,3-Triazole-based Inhibitors of the VIM-2 Metallo-β-Lactamase: Synthesis and Structure-Activity Studies.

Weide Timo T Saldanha S Adrian SA Minond Dmitriy D Spicer Timothy P TP Fotsing Joseph R JR Spaargaren Michael M Frère Jean-Marie JM Bebrone Carine C Sharpless K Barry KB Hodder Peter S PS Fokin Valery V VV

ACS medicinal chemistry letters 20100701 4

Metallo-ß-lactamases (MBL) are an emerging cause of bacterial resistance to antibiotic treatment. The VIM-2 ß-lactamase is the most commonly encountered MBL in clinical isolates worldwide. Described here are potent and selective small molecule inhibitors of VIM-2 containing the arylsulfonyl-NH-1,2,3-triazole chemotype that potentiate the efficacy of the ß-lactam, imipenem, in E. coli. ...[more]

PMID: 20625539

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Discovery of [1,2,4]Triazole Derivatives as New Metallo-β-Lactamase Inhibitors.

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Project description: Not available

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