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Substituted 2-pyridinemethanol derivatives as potent and selective phosphodiesterase-4 inhibitors |
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| Authors: | Ducharme Yves Friesen Richard W Blouin Marc Côté Bernard Dubé Daniel Ethier Diane Frenette Richard Laliberté France Mancini Joseph A Masson Paul Styhler Angela Young Robert N Girard Yves |
| Affiliation: | Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire-Dorval, Québec, Canada H9R 4P8. yves_ducharme@merck.com |
| 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. |
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