Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP3 antagonists

被引：21

作者：

Belley, M ^{[1
]}

Gallant, M ^{[1
]}

Roy, B ^{[1
]}

Houde, K ^{[1
]}

Lachance, N ^{[1
]}

Labelle, M ^{[1
]}

Trimble, LA ^{[1
]}

Chauret, N ^{[1
]}

Li, C ^{[1
]}

Sawyer, N ^{[1
]}

Tremblay, N ^{[1
]}

Lamontagne, S ^{[1
]}

Carrière, MC ^{[1
]}

Denis, D ^{[1
]}

Greig, GM ^{[1
]}

Slipetz, D ^{[1
]}

Metters, KM ^{[1
]}

Gordon, R ^{[1
]}

Chan, CC ^{[1
]}

Zamboni, RJ ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 03期

关键词：

PGE(2); EP3 receptor antagonist;

D O I：

10.1016/j.bmcl.2004.11.051

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E, receptors evaluated. Many of them are very potent and selective EP3 antagonists (K-i 3-10 nM), while compound 9 is a very good and selective EP2 agonist (K-i 8 nM). The biological profile of the EP2 agonist 9 in vivo and the metabolic profile of selected EP3 antagonists are also reported. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：527 / 530

页数：4

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