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  • Title: 3-Aryl-4-methyl-2-quinolones targeting multiresistant Staphylococcus aureus bacteria.
    Author: Doléans-Jordheim A, Veron JB, Fendrich O, Bergeron E, Montagut-Romans A, Wong YS, Furdui B, Freney J, Dumontet C, Boumendjel A.
    Journal: ChemMedChem; 2013 Apr; 8(4):652-7. PubMed ID: 23436688.
    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.
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