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ID: ALA1136524

Journal: Bioorg Med Chem Lett

Title: Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors.

Authors: Ducharme Y, Friesen RW, Blouin M, Côté B, Dubé D, Ethier D, Frenette R, Laliberté F, Mancini JA, Masson P, Styhler A, Young RN, Girard Y.

Abstract: The synthesis and the phosphodiesterase-4 (PDE4) inhibitory activity of 2-pyridinemethanol derivatives is described. The evaluation of the structure-activity relationship (SAR) in this series of novel PDE4 inhibitors led to the identification of compound 9 which exhibits excellent in vitro activity, desirable pharmacokinetic parameters and good efficacy in animal models of bronchoconstriction.

CiteXplore: 12749899

DOI: 10.1016/s0960-894x(03)00314-7