Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP4 receptor

被引：16

作者：

Burch, Jason D. ^{[1
]}

Belley, Michel ^{[1
]}

Fortin, Rejean ^{[1
]}

Deschenes, Denis ^{[1
]}

Girard, Mario ^{[1
]}

Colucci, John ^{[1
]}

Farand, Julie ^{[1
]}

Therien, Alex G. ^{[1
]}

Mathieu, Marie-Claude ^{[1
]}

Denis, Danielle ^{[1
]}

Vigneault, Erika ^{[1
]}

Levesque, Jean-Francois ^{[1
]}

Gagne, Sebastien ^{[1
]}

Wrona, Mark ^{[1
]}

Xu, Diagen ^{[1
]}

Clark, Patsy ^{[1
]}

Rowland, Steve ^{[1
]}

Han, Yongxin ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Kirkland, PQ H9H 3L1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 06期

关键词：

D O I：

10.1016/j.bmcl.2008.01.103

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of EP4 antagonists based on a quinoline acylsulfonamide scaffold have been identified as part of our ongoing efforts to develop treatments for chronic inflammation. These compounds show subnanomolar intrinsic binding potency towards the EP4 receptor, and excellent selectivity towards other prostanoid receptors. Acceptable pharmacokinetic profiles have also been demonstrated across a series of preclinical species. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2048 / 2054

页数：7

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