Antibacterial activity of quinoxalines, quinazolines, and 1,5-naphthyridines

Bioorg Med Chem Lett. 2013 Sep 1;23(17):4968-74. doi: 10.1016/j.bmcl.2013.06.048. Epub 2013 Jun 26.

Abstract

Several phenyl substituted naphthalenes and isoquinolines have been identified as antibacterial agents that inhibit FtsZ-Zing formation. In the present study we evaluated the antibacterial of several phenyl substituted quinoxalines, quinazolines and 1,5-naphthyridines against methicillin-sensitive and methicillin-resistant Staphylococcusaureus and vancomycin-sensitive and vancomycin-resistant Enterococcusfaecalis. Some of the more active compounds against S. aureus were evaluated for their effect on FtsZ protein polymerization. Further studies were also performed to assess their relative bactericidal and bacteriostatic activities. The notable differences observed between nonquaternized and quaternized quinoxaline derivatives suggest that differing mechanisms of action are associated with their antibacterial properties.

Keywords: 1,5-Naphthyridines; Antibiotics; Bactericidal; Bacteriostatic; Enterococcus faecalis; Quinazolines; Quinoxalines; Staphylococcus aureus.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Drug Resistance, Bacterial
  • Enterococcus faecalis / drug effects*
  • Gram-Positive Bacterial Infections / drug therapy
  • Humans
  • Methicillin Resistance
  • Microbial Sensitivity Tests
  • Naphthyridines / chemistry
  • Naphthyridines / pharmacology*
  • Quinazolines / chemistry
  • Quinazolines / pharmacology*
  • Quinoxalines / chemistry
  • Quinoxalines / pharmacology*
  • Staphylococcal Infections / drug therapy
  • Staphylococcus aureus / drug effects*
  • Vancomycin / pharmacology

Substances

  • Anti-Bacterial Agents
  • Naphthyridines
  • Quinazolines
  • Quinoxalines
  • Vancomycin