title: Azaindoles as potent CRTH2 receptor antagonists.
abstract: A new class of 7-azaindole analogs of MK-7246 as potent and selective CRTH2 antagonists is reported. The SAR leading to the identification of the optimal azaindole regioisomer as well as the pharmacokinetics and off-target activities of the most potent antagonists are disclosed.
authors.affiliation: Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec, Canada H9H 3L1. daniel.simard@merck.com
authors.forename: Daniel
authors.initials: D
authors.lastname: Simard
authors.forename: Yves
authors.initials: Y
authors.lastname: Leblanc
authors.forename: Carl
authors.initials: C
authors.lastname: Berthelette
authors.forename: M Helmi
authors.initials: MH
authors.lastname: Zaghdane
authors.forename: Carmela
authors.initials: C
authors.lastname: Molinaro
authors.forename: Zhaoyin
authors.initials: Z
authors.lastname: Wang
authors.forename: Michel
authors.initials: M
authors.lastname: Gallant
authors.forename: Stephen
authors.initials: S
authors.lastname: Lau
authors.forename: Trinh
authors.initials: T
authors.lastname: Thao
authors.forename: Martine
authors.initials: M
authors.lastname: Hamel
authors.forename: Rino
authors.initials: R
authors.lastname: Stocco
authors.forename: Nicole
authors.initials: N
authors.lastname: Sawyer
authors.forename: Susan
authors.initials: S
authors.lastname: Sillaots
authors.forename: Francois
authors.initials: F
authors.lastname: Gervais
authors.forename: Robert
authors.initials: R
authors.lastname: Houle
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Lévesque
mesh_terms: D000818:Animals; D002243:Carbolines / Q000737:chemistry; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: C554899:((7R)-7-(((4-fluorophenyl)sulfonyl)(methyl)amino)-6,7,8,9-tetrahydropyrido(1,2-a)indol-10-yl)acetic acid; C023422:7-azaindole dimer; D002243:Carbolines; D007211:Indoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C036293:prostaglandin D2 receptor