等排体雷马曲班类似物：选择性强效半胱氨酰白三烯受体2拮抗剂。

Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.

作者信息

Robarge Michael J, Bom David C, Tumey L Nathan, Varga Norbert, Gleason Elizabeth, Silver Daniel, Song Jianping, Murphy Steven M, Ekema George, Doucette Chris, Hanniford Doug, Palmer Marc, Pawlowski Gary, Danzig Joel, Loftus Margaret, Hunady Karen, Sherf Bruce A, Mays Robert W, Stricker-Krongrad Alain, Brunden Kurt R, Harrington John J, Bennani Youssef L

机构信息

Athersys, Inc., Medicinal Chemistry, 3201 Carnegie Avenue, Cleveland, OH 44115-2634, USA.

出版信息

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1749-53. doi: 10.1016/j.bmcl.2004.12.055.

DOI:10.1016/j.bmcl.2004.12.055

PMID:15745833

Abstract

The chemoattractant receptor-homologous molecule expressed on T(H)2 cells (CRTH-2), also found on eosinophils and basophils, is a prostaglandin D2 receptor involved in the recruitment of these cell types during an inflammatory response. In this report, we describe the synthesis and optimization of a ramatroban isostere that is a selective and potent antagonist of CRTH-2 which may be useful in the treatment of certain diseases.

摘要

辅助性T细胞2（TH2）上表达的趋化因子受体同源分子（CRTH-2），也存在于嗜酸性粒细胞和嗜碱性粒细胞上，是一种前列腺素D2受体，在炎症反应期间参与这些细胞类型的募集。在本报告中，我们描述了一种雷马曲班类似物的合成与优化，该类似物是一种选择性强效CRTH-2拮抗剂，可能对某些疾病的治疗有用。