Diaryl piperidines as CB1 receptor antagonists.
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.
Scott
Jack D
JD
Department of Medicinal Chemistry, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. jack.scott@spcorp.com
Li
Sarah W
SW
Wang
Hongwu
H
Xia
Yan
Y
Jayne
Charles L
CL
Miller
Michael W
MW
Duffy
Ruth A
RA
Boykow
George C
GC
Kowalski
Timothy J
TJ
Spar
Brian D
BD
Stamford
Andrew W
AW
Chackalamannil
Samuel
S
Lachowicz
Jean E
JE
Greenlee
William J
WJ
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
D010880:Piperidines; D043884:Receptor, Cannabinoid, CB1