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3-Aryl-4-methyl-2-quinolones Targeting Multiresistant Staphylococcus aureus Bacteria

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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https://hal-univ-lyon1.archives-ouvertes.fr/hal-02522196
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Submitted on : Friday, March 27, 2020 - 5:57:50 PM
Last modification on : Friday, July 17, 2020 - 8:28:03 AM

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Anne Doléans-Jordheim, J. B. Veron, Olivier Fendrich, Emmanuel Bergeron, A. Montagut-Romans, et al.. 3-Aryl-4-methyl-2-quinolones Targeting Multiresistant Staphylococcus aureus Bacteria. ChemMedChem, Wiley-VCH Verlag, 2013, ⟨10.1002/cmdc.201200551⟩. ⟨hal-02522196⟩

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