4.5 Article

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

Journal

ACS MEDICINAL CHEMISTRY LETTERS
Volume 1, Issue 4, Pages 150-154

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ml900022q

Keywords

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

Funding

  1. National Institutes of Health [NS059451, GM087620]
  2. Skaggs Institute for Chemical Biology

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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.

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