title: The discovery of novel indole-2-carboxamides as cannabinoid CB(1) receptor antagonists.
abstract: The discovery and structure-activity relationship of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 26i was found to be a high potency, selective cannabinoid CB(1) antagonist.
authors.affiliation: Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK. phillip.cowley@merck.com
authors.forename: Phillip M
authors.initials: PM
authors.lastname: Cowley
authors.forename: James
authors.initials: J
authors.lastname: Baker
authors.forename: David R
authors.initials: DR
authors.lastname: Barn
authors.forename: Kirsteen I
authors.initials: KI
authors.lastname: Buchanan
authors.forename: Ian
authors.initials: I
authors.lastname: Carlyle
authors.forename: John K
authors.initials: JK
authors.lastname: Clark
authors.forename: Thomas R
authors.initials: TR
authors.lastname: Clarkson
authors.forename: Maureen
authors.initials: M
authors.lastname: Deehan
authors.forename: Darren
authors.initials: D
authors.lastname: Edwards
authors.forename: Richard R
authors.initials: RR
authors.lastname: Goodwin
authors.forename: David
authors.initials: D
authors.lastname: Jaap
authors.forename: Yasuko
authors.initials: Y
authors.lastname: Kiyoi
authors.forename: Chris
authors.initials: C
authors.lastname: Mort
authors.forename: Ronald
authors.initials: R
authors.lastname: Palin
authors.forename: Alan
authors.initials: A
authors.lastname: Prosser
authors.forename: Glenn
authors.initials: G
authors.lastname: Walker
authors.forename: Nick
authors.initials: N
authors.lastname: Ward
authors.forename: Grant
authors.initials: G
authors.lastname: Wishart
authors.forename: Trevor
authors.initials: T
authors.lastname: Young
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D000818:Animals; D004285:Dogs; D004353:Drug Evaluation, Preclinical; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D008297:Male; D051379:Mice; D008958:Models, Molecular; D051381:Rats; D017208:Rats, Wistar; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D007211:Indoles; D043884:Receptor, Cannabinoid, CB1