title: Diaryl piperidines as CB1 receptor antagonists.
abstract: The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jack.scott@spcorp.com
authors.forename: Jack D
authors.initials: JD
authors.lastname: Scott
authors.forename: Sarah W
authors.initials: SW
authors.lastname: Li
authors.forename: Hongwu
authors.initials: H
authors.lastname: Wang
authors.forename: Yan
authors.initials: Y
authors.lastname: Xia
authors.forename: Charles L
authors.initials: CL
authors.lastname: Jayne
authors.forename: Michael W
authors.initials: MW
authors.lastname: Miller
authors.forename: Ruth A
authors.initials: RA
authors.lastname: Duffy
authors.forename: George C
authors.initials: GC
authors.lastname: Boykow
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Kowalski
authors.forename: Brian D
authors.initials: BD
authors.lastname: Spar
authors.forename: Andrew W
authors.initials: AW
authors.lastname: Stamford
authors.forename: Samuel
authors.initials: S
authors.lastname: Chackalamannil
authors.forename: Jean E
authors.initials: JE
authors.lastname: Lachowicz
authors.forename: William J
authors.initials: WJ
authors.lastname: Greenlee
mesh_terms: D000818:Animals; D004032:Diet / Q000009:adverse effects; D004435:Eating / Q000187:drug effects / Q000502:physiology; D051379:Mice; D008820:Mice, Obese; D009765:Obesity / Q000209:etiology / Q000378:metabolism; D010880:Piperidines / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D011485:Protein Binding / Q000502:physiology; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D010880:Piperidines; D043884:Receptor, Cannabinoid, CB1