3‐Aryl‐4‐methyl‐2‐quinolones Targeting Multiresistant Staphylococcus aureus Bacteria. Issue 4 (21st February 2013)

• Record Type: Journal Article
• Authors: Doléans‐Jordheim, Anne; Veron, Jean‐Baptiste; Fendrich, Olivier; Bergeron, Emmanuelle; Montagut‐Romans, Adrien; Wong, Yung‐Sing; Furdui, Bianca; Freney, Jean; Dumontet, Charles; Boumendjel, Ahcène
• Is Part Of: ChemMedChem. Volume 8:Issue 4(2013:Apr.)
• Page Start: 652
• Page End: 657
• Publication Date: 2013-02-21
• Subjects: Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.1002/cmdc.201200551
• Languages: English
• ISSNs: 1860-7179

Abstract

<abstract abstract-type="main" xml:lang="en"> <title>Abstract</title> <p>The NorA efflux pump lowers intracellular fluoroquinolone concentrations by expelling antibiotics through the membrane of <italic>Staphylococcus aureus</italic>. We identified 3‐aryl‐4‐methyl‐2‐quinolin‐2‐ones as compounds able to restore the activity of the NorA substrate, ciprofloxacin, against resistant <italic>S. aureus</italic> strains, and acting as efflux pump inhibitors (EPI). In particular, 5‐hydroxy‐7‐methoxy‐4‐methyl‐3‐phenylquinolin‐2‐one (<bold>6 c</bold>) presents both an EPI and an antimicrobial effect. Its efficacy and safety make it a potential candidate for further investigations.</p> </abstract>