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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:23

Article

Parhi, Ajit K.^1,2  Zhang, Yongzheng²  Saionz, Kurt W.²  Pradhan, Padmanava^3,4  Kaul, Malvika⁵  Trivedi, Kalkal⁵  Pilch, Daniel S.⁵  LaVoie, Edmond J.¹ 

[1] Rutgers State Univ, Dept Med Chem, Piscataway, NJ 08854 USA

[2] TAXIS Pharmaceut Inc, North Brunswick, NJ USA

[3] City Coll, Dept Chem, New York, NY 10031 USA

[4] CUNY, New York, NY 10031 USA

[5] Univ Med & Dent New Jersey, Robert Wood Johnson Med Sch, Dept Pharmacol, Piscataway, NJ 08854 USA

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

DOI  :  10.1016/j.bmcl.2013.06.048

来源: Elsevier

【 摘 要 】

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.

【 授权许可】

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