3-Aryl-4-methyl-2-quinolones Targeting Multiresistant Staphylococcus aureus Bacteria - Archive ouverte HAL Access content directly
Journal Articles ChemMedChem Year : 2013

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

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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.

Dates and versions

hal-02522196 , version 1 (27-03-2020)

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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, 2013, ⟨10.1002/cmdc.201200551⟩. ⟨hal-02522196⟩
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