title: Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.
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.
authors.affiliation: Athersys, Inc., Medicinal Chemistry, 3201 Carnegie Avenue, Cleveland, OH 44115-2634, USA. mrobarge@athersys.com
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Robarge
authors.forename: David C
authors.initials: DC
authors.lastname: Bom
authors.forename: L Nathan
authors.initials: LN
authors.lastname: Tumey
authors.forename: Norbert
authors.initials: N
authors.lastname: Varga
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Gleason
authors.forename: Daniel
authors.initials: D
authors.lastname: Silver
authors.forename: Jianping
authors.initials: J
authors.lastname: Song
authors.forename: Steven M
authors.initials: SM
authors.lastname: Murphy
authors.forename: George
authors.initials: G
authors.lastname: Ekema
authors.forename: Chris
authors.initials: C
authors.lastname: Doucette
authors.forename: Doug
authors.initials: D
authors.lastname: Hanniford
authors.forename: Marc
authors.initials: M
authors.lastname: Palmer
authors.forename: Gary
authors.initials: G
authors.lastname: Pawlowski
authors.forename: Joel
authors.initials: J
authors.lastname: Danzig
authors.forename: Margaret
authors.initials: M
authors.lastname: Loftus
authors.forename: Karen
authors.initials: K
authors.lastname: Hunady
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Sherf
authors.forename: Robert W
authors.initials: RW
authors.lastname: Mays
authors.forename: Alain
authors.initials: A
authors.lastname: Stricker-Krongrad
authors.forename: Kurt R
authors.initials: KR
authors.lastname: Brunden
authors.forename: John J
authors.initials: JJ
authors.lastname: Harrington
authors.forename: Youssef L
authors.initials: YL
authors.lastname: Bennani
mesh_terms: D018927:Anti-Asthmatic Agents / Q000737:chemistry / Q000494:pharmacology; D002227:Carbazoles / Q000737:chemistry* / Q000494:pharmacology*; D007536:Isomerism; D008956:Models, Chemical; D008968:Molecular Conformation; D015394:Molecular Structure; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D018927:Anti-Asthmatic Agents; D002227:Carbazoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; D013449:Sulfonamides; C063119:ramatroban; C036293:prostaglandin D2 receptor