discovery of quinoline small molecules with potent dispersal activity against methicillin-resistant staphylococcus aureus and staphylococcus epidermidis biofilms using a scaffold hopping strategy：（发现喹啉衍生物小分子与强有力的传播活动对耐甲氧西林金黄色葡萄球菌和葡萄球菌epiderm）.pdfVIP

Bioorganic Medicinal Chemistry Letters 24 (2014) 5076–5080 Contents lists available at ScienceDirect Bioorganic Medicinal Chemistry Letters journal homepage: /locate/bmcl Discovery of quinoline small molecules with potent dispersal activity against methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis biofilms using a scaffold hopping strategy Yasmeen Abouelhassan, Aaron T. Garrison, Gena M. Burch, Wilson Wong, Verrill M. Norwood IV, Robert W. Huigens III ⇑ University of Florida, Department of Medicinal Chemistry, College of Pharmacy, 1600 SW Archer Rd., Gainesville, FL 32610, USA a r t i c l e i n f o a b s t r a c t Article history: Staphylococcus aureus and Staphylococcus epidermidis are recognized as the most frequent cause of bio- Received 14 August 2014 film-associated nosocomial and indwelling medical device infections. Biofilm-associated infections are Revised 30 August 2014 known to be highly resistant to our current arsenal of clinically used antibiotics and antibacterial agents. Accepted 2 September 2014 To exacerbate this problem, no therapeutic option exists that targets biofilm-dependent machinery crit- Available online 15 September 2014 ical 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 Keywords: S. aureus and S