title: Novel benzimidazole-based MCH R1 antagonists.
abstract: The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity.
authors.affiliation: Metabolic and Viral Diseases Centre of Excellence for Drug Discovery, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709, USA. andrew.j.carpenter@gsk.com
authors.forename: Andrew J
authors.initials: AJ
authors.lastname: Carpenter
authors.forename: Kamal A
authors.initials: KA
authors.lastname: Al-Barazanji
authors.forename: Kevin K
authors.initials: KK
authors.lastname: Barvian
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Bishop
authors.forename: Christy S
authors.initials: CS
authors.lastname: Britt
authors.forename: Joel P
authors.initials: JP
authors.lastname: Cooper
authors.forename: Aaron S
authors.initials: AS
authors.lastname: Goetz
authors.forename: Mary K
authors.initials: MK
authors.lastname: Grizzle
authors.forename: Donald L
authors.initials: DL
authors.lastname: Hertzog
authors.forename: Diane M
authors.initials: DM
authors.lastname: Ignar
authors.forename: Ronda O
authors.initials: RO
authors.lastname: Morgan
authors.forename: Gregory E
authors.initials: GE
authors.lastname: Peckham
authors.forename: Jason D
authors.initials: JD
authors.lastname: Speake
authors.forename: Will R
authors.initials: WR
authors.lastname: Swain
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000493:pharmacokinetics / Q000494:pharmacology*; D001682:Biological Availability; D001823:Body Composition; D004305:Dose-Response Relationship, Drug; D051379:Mice; D023421:Models, Animal; D009765:Obesity / Q000188:drug therapy*; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D015431:Weight Loss / Q000187:drug effects
chemical_list: D001562:Benzimidazoles; C491209:Mchr1 protein, mouse; D017481:Receptors, Somatostatin; C031000:benzimidazole