3-吲哚基砜作为选择性 CRTh2 拮抗剂。
3-Indolyl sultams as selective CRTh2 antagonists.
机构信息
Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA.
出版信息
Bioorg Med Chem Lett. 2010 Jun 1;20(11):3287-90. doi: 10.1016/j.bmcl.2010.04.046. Epub 2010 Apr 14.
PMID:20457519
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).
摘要
CRTh2（DP(2)）是一种前列腺素 D(2) 受体，参与招募哮喘肺部中的嗜酸性粒细胞和嗜碱性粒细胞。在这里，我们报告了一系列新型 3-吲哚基磺酰胺拮抗剂的发现，它们对 CRTh2 的亲和力低至纳摩尔级。这些化合物被证明对其他主要的前列腺素 D(2) 受体（DP1）以及血栓素 A(2) 受体（TP）具有选择性。
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