Design and synthesis of novel antibacterial agents with inhibitory activity against DNA polymerase III

Bioorg Med Chem Lett. 2001 Aug 20;11(16):2185-8. doi: 10.1016/s0960-894x(01)00407-3.

Abstract

4-Substituted 2-amino-6-(anilino)pyrimidines have been found to be selective inhibitors of DNA polymerase III, a replicative enzyme known to be essential in the DNA synthesis of Gram-positive bacteria. Among the analogues, 18 displayed an IC(50) of 10 microM against DNA polymerase III from Staphylococcus aureus.

MeSH terms

  • Aniline Compounds / chemical synthesis*
  • Aniline Compounds / chemistry
  • Aniline Compounds / pharmacology
  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • DNA Polymerase III / antagonists & inhibitors*
  • DNA Polymerase III / metabolism
  • Drug Design
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Microbial Sensitivity Tests
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology
  • Staphylococcus aureus / drug effects
  • Staphylococcus aureus / enzymology
  • Structure-Activity Relationship

Substances

  • Aniline Compounds
  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Pyrimidines
  • DNA Polymerase III