3,4-Disubstituted indole acylsulfonamides: A novel series of potent and selective human EP3 receptor antagonists

被引：40

作者：

Zhou, Nian ^{[1
]}

Zeller, Wayne ^{[1
]}

Krohn, Michael ^{[1
]}

Anderson, Herb ^{[1
]}

Zhang, Jun ^{[1
]}

Onua, Emmanuel ^{[1
]}

Kiselyov, Alex S. ^{[1
]}

Ramirez, Jose ^{[2
]}

Halldorsdottir, Gulrun ^{[2
]}

Andresson, Porkell ^{[2
]}

Gurney, Mark E. ^{[2
]}

Singh, Jasbir ^{[1
]}

机构：

[1] deCODE Chem Inc, Dept Med Chem, Woodridge, IL 60517 USA

[2] deCODE Genet Inc, Reykjavik, Iceland

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 01期

关键词：

Prostanoid receptor antagonists; EP3 receptor antagonists; Peri-substituted indoles; Acylsulfonamides; ANALOGS; PROSTAGLANDIN-E2; CYCLASE; CELLS;

D O I：

10.1016/j.bmcl.2008.11.007

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of potent and selective EP3 receptor antagonists are described. Utilizing a pharmacophore model developed for the EP3 receptor, a series of 3,4-disubstituted indoles were shown to be high affinity ligands for this target. These compounds showed high selectivity over IP, FP and other EP receptors and are potent antagonists in functional assays. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：123 / 126

页数：4

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