Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2

被引：43

作者：

Armer, RE

Ashton, MR

Boyd, EA

Brennan, CJ

Brookfield, FA

Gazi, L

Gyles, SL

Hay, PA

Hunter, MG

Middlemiss, D

Whittaker, M

Xue, LZ

Pettipher, R

机构：

[1] Oxagen Ltd, Abingdon OX14 4RY, Oxon, England

[2] Evotec OAI, Abingdon OX14 4RY, Oxon, England

[3] XaviaPharm, Bishops Stortford CM23 3NF, Herts, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 20期

关键词：

D O I：

10.1021/jm050519b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Prostaglandin D-2 (PGD(2)) acting at the CRTH2 receptor (chemoattractant receptor-homologous molecule expressed on Th2 cells) has been linked with a variety of allergic and other inflammatory diseases. We describe a family of indole-1-sulfonyl-3-acetic acids that are potent and selective CRTH2 antagonists that possess good oral bioavailability. The compounds may serve as novel starting points for the development of treatments of inflammatory disease such as asthma, allergic rhinitis, and atopic dermatitis.

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收藏

页码：6174 / 6177

页数：4

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