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