Phenyl thiazolyl urea and carbamate derivatives as new inhibitors of bacterial cell-wall biosynthesis

Bioorg Med Chem Lett. 2004 Jan 5;14(1):235-8. doi: 10.1016/j.bmcl.2003.09.082.

Abstract

Over 50 phenyl thiazolyl urea and carbamate derivatives were synthesized for evaluation as new inhibitors of bacterial cell-wall biosynthesis. Many of them demonstrated good activity against MurA and MurB and gram-positive bacteria including MRSA, VRE and PRSP. 3,4-Difluorophenyl 5-cyanothiazolylurea (3p) with clog P of 2.64 demonstrated antibacterial activity against both gram-positive and gram-negative bacteria.

MeSH terms

  • Anti-Bacterial Agents / pharmacology*
  • Carbamates / chemistry*
  • Carbamates / pharmacology*
  • Cell Wall / drug effects
  • Cell Wall / enzymology
  • Enterococcus faecalis / drug effects
  • Enterococcus faecalis / enzymology
  • Escherichia coli / drug effects
  • Escherichia coli / enzymology
  • Microbial Sensitivity Tests
  • Peptidoglycan / biosynthesis*
  • Phenylthiazolylthiourea / analogs & derivatives*
  • Phenylthiazolylthiourea / pharmacology*
  • Staphylococcus / drug effects
  • Staphylococcus / enzymology

Substances

  • Anti-Bacterial Agents
  • Carbamates
  • Peptidoglycan
  • Phenylthiazolylthiourea