These authors contributed equally to this work.
3-Aryl-4-methyl-2-quinolones Targeting Multiresistant Staphylococcus aureus Bacteria
Version of Record online: 21 FEB 2013
Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Special Issue: Obesity, Diabetes and Metabolic Syndrome
Volume 8, Issue 4, pages 652–657, April 2013
How to Cite
Doléans-Jordheim, A., Veron, J.-B., Fendrich, O., Bergeron, E., Montagut-Romans, A., Wong, Y.-S., Furdui, B., Freney, J., Dumontet, C. and Boumendjel, A. (2013), 3-Aryl-4-methyl-2-quinolones Targeting Multiresistant Staphylococcus aureus Bacteria. ChemMedChem, 8: 652–657. doi: 10.1002/cmdc.201200551
- Issue online: 25 MAR 2013
- Version of Record online: 21 FEB 2013
- Manuscript Received: 28 NOV 2012
- efflux pumps;
The NorA efflux pump lowers intracellular fluoroquinolone concentrations by expelling antibiotics through the membrane of Staphylococcus aureus. We identified 3-aryl-4-methyl-2-quinolin-2-ones as compounds able to restore the activity of the NorA substrate, ciprofloxacin, against resistant S. aureus strains, and acting as efflux pump inhibitors (EPI). In particular, 5-hydroxy-7-methoxy-4-methyl-3-phenylquinolin-2-one (6 c) presents both an EPI and an antimicrobial effect. Its efficacy and safety make it a potential candidate for further investigations.