Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors

Potent inhibitors of the human PDE IV enzyme are described. Substituted 8-arylquinoline analogs bearing nitrogen-linked side chain were identified as potent inhibitors based on the SAR described herein. Potent inhibitors of the human PDE IV enzyme are described. Substituted 8-arylquinoline analogs b...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-05, Vol.16 (10), p.2608-2612
Hauptverfasser: Lacombe, Patrick, Deschênes, Denis, Dubé, Daniel, Dubé, Laurence, Gallant, Michel, Macdonald, Dwight, Mastracchio, Antony, Perrier, Hélène, Charleson, Stella, Huang, Zheng, Laliberté, France, Liu, Susana, Mancini, Joseph A., Masson, Paul, Salem, Myriam, Styhler, Angela, Girard, Yves
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Sprache:eng
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Zusammenfassung:Potent inhibitors of the human PDE IV enzyme are described. Substituted 8-arylquinoline analogs bearing nitrogen-linked side chain were identified as potent inhibitors based on the SAR described herein. Potent inhibitors of the human PDE IV enzyme are described. Substituted 8-arylquinoline analogs bearing nitrogen-linked side chain were identified as potent inhibitors based on the SAR described herein. The pharmacokinetic profile of the best analog and the in vivo efficacy in an ovalbumin-induced bronchoconstriction assay in conscious guinea pigs are reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.02.043