Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists

…, D Hanniford, M Palmer, G Pawlowski, J Danzig…

Index: 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. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 6 p. 1749 - 1753

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Citation Number: 27

Abstract

The chemoattractant receptor-homologous molecule expressed on TH2 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.