Development of improved inhibitors of wall teichoic acid biosynthesis with potent activity against Staphylococcus aureus

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1767-70. doi: 10.1016/j.bmcl.2010.01.036. Epub 2010 Jan 20.

Abstract

A small molecule (1835F03) that inhibits Staphylococcus aureus wall teichoic acid biosynthesis, a proposed antibiotic target, has been discovered. Rapid, parallel, solution-phase synthesis was employed to generate a focused library of analogs, providing detailed information about structure-activity relationships and leading to the identification of targocil, a potent antibiotic.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Microbial Sensitivity Tests
  • Quinazolines / chemical synthesis
  • Quinazolines / chemistry
  • Quinazolines / pharmacology
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship
  • Teichoic Acids / biosynthesis*
  • Teichoic Acids / metabolism

Substances

  • Anti-Bacterial Agents
  • Quinazolines
  • Teichoic Acids