Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors

被引：4

作者：

Lacombe, P ^{[1
]}

Deschênes, D ^{[1
]}

Dubé, D ^{[1
]}

Dubé, L ^{[1
]}

Gallant, M ^{[1
]}

Macdonald, D ^{[1
]}

Mastracchlo, A ^{[1
]}

Perrier, H ^{[1
]}

Charleson, S ^{[1
]}

Huang, Z ^{[1
]}

Laliberté, F ^{[1
]}

Liu, S ^{[1
]}

Mancini, JA ^{[1
]}

Masson, P ^{[1
]}

Salem, M ^{[1
]}

Styhler, A ^{[1
]}

Girard, Y ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 10期

关键词：

PDE4; TNF-alpha; c-AMP; asthma; COPD;

D O I：

10.1016/j.bmcl.2006.02.043

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 ail ovalbumin-induced bronchoconstriction assay in conscious guinea pigs are reported. (C) 2006 Elsevier Ltd. All rights reserved.

引用

页码：2608 / 2612

页数：5

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