Inhibitors of the bacterial cell wall biosynthesis enzyme MurC

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1451-4. doi: 10.1016/s0960-894x(01)00251-7.

Abstract

A series of phosphinate transition-state analogues of the L-alanine adding enzyme (MurC) of bacterial peptidoglycan biosynthesis was prepared and tested as inhibitors of the Escherichia coli enzyme. Compound 4 was identified as a potent inhibitor of MurC from Escherichia coli with an IC(50) of 49nM.

MeSH terms

  • Cell Wall / drug effects*
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Escherichia coli / drug effects
  • Escherichia coli / enzymology*
  • Peptide Synthases / antagonists & inhibitors*
  • Peptide Synthases / metabolism
  • Peptidoglycan / metabolism

Substances

  • Enzyme Inhibitors
  • Peptidoglycan
  • Peptide Synthases
  • UDP-N-acetylmuramoyl-alanine synthetase