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

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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 Staphylococcus aureus and vancomycin-sensitive and vancomycin-resistant Enterococcus faecalis. 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.

Original languageEnglish (US)
Pages (from-to)4968-4974
Number of pages7
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number17
DOIs
StatePublished - Sep 1 2013

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Keywords

  • 1,5-Naphthyridines
  • Antibiotics
  • Bactericidal
  • Bacteriostatic
  • Enterococcus faecalis
  • Quinazolines
  • Quinoxalines
  • Staphylococcus aureus

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