1392191-08-0Relevant articles and documents
NOVEL AZACOUMARIN DERIVATIVES HAVING MDR PUMP INHIBITING ACTIVITY
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Paragraph 0101-0102; 0115; 0116; 0141 - 0144, (2014/02/16)
The present invention relates to compounds of formula (I), where R1 and R2, identical or different, are each independently a hydrogen atom or a non-substituted or substituted (C1-C12) alkyl group; R3 is a hydrogen atom or a non-substituted or substituted (C1-C6) alkyl group; R4 is a non-substituted or substituted (C1-C12) alkyl group or an aryl or heteroaryl group, said aryl and heteroaryl groups being non-substituted or substituted; and R5 is a non-substituted or substituted (C1-C12) alkyl group; or R4 and R5 are bonded to one another by a saturated hydrocarbon chain having 3 or 4 carbon atoms, optionally in hydrated form or in the form of a salt that is acceptable for being administered to animals or plants, for the use thereof as a potentiator of the effect of an antimicrobial agent or for the use thereof as an antimicrobial agent.
3-Aryl-4-methyl-2-quinolones Targeting Multiresistant Staphylococcus aureus Bacteria
Doleans-Jordheim, Anne,Veron, Jean-Baptiste,Fendrich, Olivier,Bergeron, Emmanuelle,Montagut-Romans, Adrien,Wong, Yung-Sing,Furdui, Bianca,Freney, Jean,Dumontet, Charles,Boumendjel, Ahcene
, p. 652 - 657 (2013/08/22)
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 (6c) presents both an EPI and an antimicrobial effect. Its efficacy and safety make it a potential candidate for further investigations.