3‐Aryl‐4‐methyl‐2‐quinolones Targeting Multiresistant Staphylococcus aureus Bacteria. Issue 4 (21st February 2013) - Doléans‐Jordheim, Anne
Abstract 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.