NH-1,2,3-Triazole Inhibitors of the VIM-2 Metallo-β-Lactamase

被引：83

作者：

Weide, Timo ^{[2
]}

Saldanha, S. Adrian ^{[1
]}

Minond, Dmitriy ^{[1
]}

Spicer, Timothy P. ^{[1
]}

Fotsing, Joseph R. ^{[2
]}

Spaargaren, Michael ^{[1
]}

Frere, Jean-Marie ^{[3
]}

Bebrone, Carine ^{[3
]}

Sharpless, K. Barry ^{[2
]}

Hodder, Peter S. ^{[1
]}

Fokin, Valery V. ^{[2
]}

机构：

[1] Scripps Res Inst, Translat Res Inst, Jupiter, FL 33458 USA

[2] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA

[3] Univ Liege, Ctr Prot Engn, B-4000 Liege, Belgium

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2010年 / 1卷 / 04期

基金：

美国国家卫生研究院;

关键词：

Metallo-beta-lactamases; VIM-2; NH-1,2,3-triazole-based inhibitors; bacterial resistance; Escherichia coli;

D O I：

10.1021/ml900022q

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Metallo-beta-lactamases (MBLs) are an emerging cause of bacterial resistance to antibiotic treatment. The VIM-2 beta-lactamase is the most commonly encountered MBLs 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 beta-lactam, imipenem, in Escherichia coli.

引用

页码：150 / 154

页数：5

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