NH-1,2,3-triazole inhibitors of the VIM-2 metallo-β-lactamase

Timo Weide, S. Adrian Saldanha, Dmitriy Minond, Timothy P. Spicer, Joseph R. Fotsing, Michael Spaargaren, Jean Marie Frère, Carine Bebrone, K. Barry Sharpless, Peter S. Hodder, Valery V. Fokin

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Abstract

Metallo-β-lactamases (MBLs) are an emerging cause of bacterial resistance to antibiotic treatment. The VIM-2 β-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 β-lactam, imipenem, in Escherichia coli.

Original languageEnglish
Pages (from-to)150-154
Number of pages5
JournalACS Medicinal Chemistry Letters
Volume1
Issue number4
DOIs
Publication statusPublished - 2010
Externally publishedYes

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Keywords

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

ASJC Scopus subject areas

  • Organic Chemistry
  • Drug Discovery
  • Biochemistry

Cite this

Weide, T., Saldanha, S. A., Minond, D., Spicer, T. P., Fotsing, J. R., Spaargaren, M., Frère, J. M., Bebrone, C., Sharpless, K. B., Hodder, P. S., & Fokin, V. V. (2010). NH-1,2,3-triazole inhibitors of the VIM-2 metallo-β-lactamase. ACS Medicinal Chemistry Letters, 1(4), 150-154. https://doi.org/10.1021/ml900022q