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
收藏
页码:150 / 154
页数:5
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