title: Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.
abstract: The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB(1) antagonist with high predicted human oral bioavailability.
authors.affiliation: Department of Chemistry, MSD, Newhouse, Lanarkshire ML1 5SH, UK. phillip.cowley@tppgd.com
authors.forename: Phillip M
authors.initials: PM
authors.lastname: Cowley
authors.forename: James
authors.initials: J
authors.lastname: Baker
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: Yasuko
authors.initials: Y
authors.lastname: Kiyoi
authors.forename: Iain
authors.initials: I
authors.lastname: Martin
authors.forename: Dawn
authors.initials: D
authors.lastname: Osbourn
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
mesh_terms: D000284:Administration, Oral; D001682:Biological Availability; D006801:Humans; D007211:Indoles / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D043884:Receptor, Cannabinoid, CB1