Antimicrobial quinolone derivatives and use of the same to...

Details Antimicrobial quinolone derivatives and use of the same to... Antimicrobial quinolone derivatives and use of the same to...

C - Chemistry, Metallurgy

07

D

C07D 413/12 (2006.01) A61K 31/4709 (2006.01) A61P 31/04 (2006.01) C07D 413/04 (2006.01) C07D 413/10 (2006.01) C07D 498/04 (2006.01)

Patent

CA 2424402

Substituted quinolone derivatives in which an oxazolidinone, isoxazolinone, or isoxazoline is covalently bonded to a quinolone, methods of using the quinolone derivatives, and pharmaceutical compositions containing the quinolone derivatives are disclosed. Methods of synthesizing these substituted quinolone derivatives are also disclosed, and in particular a method of manufacturing a 7-(2-oxo-1,3-oxazolidin-3-yl)aryl-3-quinolinecarboxylic acid by condensing a 4-(2-oxo-1,3-oxazolidin-5-yl)aryl boronic acid with a 7-halo- quinolone derivative. The quinolone derivatives possess antibacterial activity, and are effective against a number of human and veterinary pathogens in the treatment of bacterial diseases.

L'invention concerne des dérivés de quinolones substituée dans lesquels une oxazolidinone, une isoxazolidinone ou une isoxazoline est liée par covalence à une quinolone, des procédés d'utilisation de ces dérivés de quinolone, ainsi que des compositions pharmaceutiques contenant lesdits dérivés. L'invention concerne également des procédés de synthèse de ces dérivés de quinolone substituée et, en particulier, un procédé de fabrication d'un acide 7-(2-oxo-1,3-oxazolidine-3-yl)aryl-3-quinoléine carboxylique par condensation d'un acide 4-(2-oxo-1,3-oxazolidine-5-yl)aryl boronique avec un dérivé de 7-haloquinolone. Les dérivés de quinolone possèdent une activité antibactérienne et sont efficaces contre un grand nombre d'agents pathogènes humains et vétérinaires dans le traitement de maladies bactériennes.

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