期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 21, 页码 5076-5080出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.09.009
关键词
Drug discovery; Biofilm dispersal agent; Biofilm inhibitor; Antibacterial agent; Quinoline
资金
- Office of Research (University of Florida)
- Univ. of Florida
- College of Pharmacy
Staphylococcus aureus and Staphylococcus epidermidis are recognized as the most frequent cause of biofilm-associated nosocomial and indwelling medical device infections. Biofilm-associated infections are known to be highly resistant to our current arsenal of clinically used antibiotics and antibacterial agents. To exacerbate this problem, no therapeutic option exists that targets biofilm-dependent machinery critical to Staphylococcal biofilm formation and maintenance. Here, we describe the discovery of a series of quinoline small molecules that demonstrate potent biofilm dispersal activity against methicillin-resistant S. aureus and S. epidermidis using a scaffold hopping strategy. This interesting class of quinolines also has select synthetic analogues that demonstrate potent antibacterial activity and biofilm inhibition against S. aureus and S. epidermidis. (C) 2014 Elsevier Ltd. All rights reserved.
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