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ID: ALA1155332
Journal: Bioorg Med Chem Lett
Title: Alkyl-bridged substituted 8-arylquinolines as highly potent PDE IV inhibitors.
Authors: Lacombe P, Chauret N, Claveau D, Day S, Deschênes D, Dubé D, Gallant M, Girard Y, Huang Z, Laliberté F, Lévesque JF, Liu S, Macdonald D, Mancini JA, Masson P, Nicholson DW, Nicoll-Griffith DA, Salem M, Styhler A, Young RN.
Abstract: Substituted 8-arylquinoline analogs bearing alkyl-linked side chain were identified as potent inhibitors of type 4 phophodiesterase. These compounds address the potential liabilities of the clinical candidate L-454560. The pharmacokinetic profile of the best analogs and the in vivo efficacy in an ovalbumin-induced bronchoconstriction assay in conscious guinea pigs are reported.
CiteXplore: 19640717