Quinazolin-2-ylamino-quinazolin-4-ols as novel non-nucleoside inhibitors of bacterial DNA polymerase III

Bioorg Med Chem Lett. 2009 Feb 1;19(3):800-2. doi: 10.1016/j.bmcl.2008.12.038. Epub 2008 Dec 13.

Abstract

High throughput screening led to the discovery of a novel series of quinazolin-2-ylamino-quinazolin-4-ols as a new class of DNA polymerase III inhibitors. The inhibition of chromosomal DNA replication results in bacterial cell death. The synthesis, structure-activity relationships and functional activity are described.

MeSH terms

  • Cell Death
  • Chemistry, Pharmaceutical / methods*
  • DNA / chemistry
  • DNA Polymerase III / antagonists & inhibitors*
  • DNA Polymerase III / chemistry*
  • Drug Design
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Models, Biological
  • Models, Chemical
  • Molecular Structure
  • Quinazolines / chemistry*
  • Streptococcus pyogenes / enzymology
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Quinazolines
  • DNA
  • DNA Polymerase III