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

作者：Parhi Ajit K; Zhang Yongzheng; Saionz Kurt W; Pradhan Padmanava; Kaul Malvika; Trivedi Kalkal; Pilch Daniel S; LaVoie Edmond J^*

来源：Bioorganic & Medicinal Chemistry Letters, 2013, 23(17): 4968-4974.

DOI：10.1016/j.bmcl.2013.06.048

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

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.

• 出版日期2013-9-1