3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms

J Med Chem. 2006 Nov 2;49(22):6435-8. doi: 10.1021/jm060505l.

Abstract

The 3-aminoquinzolinediones represent a new series of antibacterial agents structurally related to the fluoroquinolones. They are inhibitors of bacterial gyrase and topoisomerase IV and demonstrate clinically useful antibacterial activity against fastidious Gram-negative and Gram-positive organisms, including multidrug- and fluoroquinolone-resistant organisms. These agents also demonstrate in vivo efficacy in murine systemic infection models.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology*
  • Bacteria / drug effects*
  • DNA Topoisomerase IV / antagonists & inhibitors
  • Drug Resistance, Multiple, Bacterial / drug effects
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Methicillin Resistance
  • Microbial Sensitivity Tests
  • Quinazolinones / chemical synthesis*
  • Structure-Activity Relationship
  • Topoisomerase II Inhibitors

Substances

  • Anti-Bacterial Agents
  • Enzyme Inhibitors
  • Quinazolinones
  • Topoisomerase II Inhibitors
  • DNA Topoisomerase IV