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Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists |
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| Authors: | 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 |
| Affiliation: | Athersys, Inc., Medicinal Chemistry, 3201 Carnegie Avenue, Cleveland, OH 44115-2634, USA. mrobarge@athersys.com |
| 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. |
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