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

被引：14

作者：

Ducharme, Y ^{[1
]}

Friesen, RW ^{[1
]}

Blouin, M ^{[1
]}

Côté, B ^{[1
]}

Dubé, D ^{[1
]}

Ethier, D ^{[1
]}

Frenette, R ^{[1
]}

Laliberté, F ^{[1
]}

Mancini, JA ^{[1
]}

Masson, P ^{[1
]}

Styhler, A ^{[1
]}

Young, RN ^{[1
]}

Girard, Y ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 11期

关键词：

D O I：

10.1016/S0960-894X(03)00314-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 broncho-constriction. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1923 / 1926

页数：4

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