3-Indolyl sultams as selective CRTh2 antagonists
L Nathan Tumey1, Michael J Robarge, Elizabeth Gleason
1Athersys, 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).
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