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Bioorg Med Chem Lett. 2010 Jun 1;20(11):3287-90. doi: 10.1016/j.bmcl.2010.04.046. Epub 2010 Apr 14.

3-Indolyl sultams as selective CRTh2 antagonists.

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1
Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA. tumeyn@wyeth.com

Abstract

CRTh2 (DP(2)) is a prostaglandin D(2) receptor implicated in the recruitment of eosinophils and basophils within the asthmatic lung. Here we report the discovery of a novel series of 3-indolyl sultam antagonists with low nM affinity for CRTh2. These compounds proved to be selective over the other primary prostaglandin D(2) receptor (DP1) as well as the thromboxane A(2) receptor (TP).

PMID:
20457519
DOI:
10.1016/j.bmcl.2010.04.046
[Indexed for MEDLINE]
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