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ID: ALA1147684

Journal: Bioorg Med Chem Lett

Title: Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.

Authors: Lacombe P, Deschênes D, Dubé D, Dubé L, Gallant M, Macdonald D, Mastracchio A, Perrier H, Charleson S, Huang Z, Laliberté F, Liu S, Mancini JA, Masson P, Salem M, Styhler A, Girard Y.

Abstract: 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.

CiteXplore: 16516471

DOI: 10.1016/j.bmcl.2006.02.043