4.5 Article

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

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 17, 页码 4968-4974

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.06.048

关键词

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

资金

  1. TAXIS Pharmaceuticals, Inc.
  2. Rutgers
  3. State University of New Jersey
  4. University of Medicine and Dentistry of New Jersey
  5. NCRR [1S10RR23698-1A1]
  6. NIH National Center for Research Resources [P41RR0954]

向作者/读者索取更多资源

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. (C) 2013 Elsevier Ltd. All rights reserved.

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