Structure-activity relationships of novel potent MurF inhibitors

Bioorg Med Chem Lett. 2004 Jan 5;14(1):267-70. doi: 10.1016/j.bmcl.2003.09.073.

Abstract

A novel class of MurF inhibitors was discovered and structure-activity relationship studies have led to several potent compounds with IC(50)=22 approximately 70 nM. Unfortunately, none of these potent MurF inhibitors exhibited significant antibacterial activity even in the presence of bacterial cell permeabilizers.

MeSH terms

  • Bacterial Proteins / antagonists & inhibitors*
  • Bacterial Proteins / metabolism
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacology*
  • Peptide Synthases / antagonists & inhibitors*
  • Peptide Synthases / metabolism
  • Peptidoglycan / biosynthesis
  • Structure-Activity Relationship

Substances

  • Bacterial Proteins
  • Enzyme Inhibitors
  • Peptidoglycan
  • Peptide Synthases
  • UDP-N-acetylmuramoylalanyl-D-glutamyllysine-D-alanyl-D-alanine ligase