Discovery of a potent and selective agonist of the prostaglandin EP4 receptor

被引：71

作者：

Billot, X ^{[1
]}

Chateauneuf, A ^{[1
]}

Chauret, N ^{[1
]}

Denis, D ^{[1
]}

Greig, G ^{[1
]}

Mathieu, MC ^{[1
]}

Metters, KM ^{[1
]}

Slipetz, DM ^{[1
]}

Young, RN ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 06期

关键词：

D O I：

10.1016/S0960-894X(03)00042-8

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Analogues of PGE(2) wherein the hydroxycyclopentanone ring has been replaced by a lactam have been prepared and evaluated as ligands for the EP4 receptor. An optimized compound (19a) shows high potency and agonist efficacy at the EP4 receptor and is highly selective over the other seven known prostaglandin receptors. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1129 / 1132

页数：4

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