title: 3-Indolyl sultams as selective CRTh2 antagonists.
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).
authors.affiliation: Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA. tumeyn@wyeth.com
authors.forename: L Nathan
authors.initials: LN
authors.lastname: Tumey
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Robarge
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Gleason
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
authors.initials: B
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: Youssef L
authors.initials: YL
authors.lastname: Bennani
authors.forename: John J
authors.initials: JJ
authors.lastname: Harrington
mesh_terms: D004951:Esterification; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D007211:Indoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; D013449:Sulfonamides; C036293:prostaglandin D2 receptor