Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.
A series of novel aminobenzimidazoles was prepared and evaluated for h-MCH-R1 antagonist properties. Most of the compounds showed excellent h-MCH-R1 binding affinity as well as mouse ex vivo binding. Compounds 9 and 18 were active in mouse DIO studies at 30mpk.
Sasikumar
T K
TK
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. thavalakulamgar.sasikumar@spcorp.com
Qiang
Li
L
Burnett
Duane A
DA
Greenlee
William J
WJ
Hawes
Brian E
BE
Kowalski
Timothy J
TJ
O'Neill
Kim
K
Spar
Brian D
BD
Weig
Blair
B
D000818:Animals; D019440:Anti-Obesity Agents / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D001667:Binding, Competitive / Q000187:drug effects; D004032:Diet; D004195:Disease Models, Animal; D004353:Drug Evaluation, Preclinical; D004435:Eating / Q000187:drug effects; D006801:Humans; D008659:Metabolic Diseases / Q000188:drug therapy*; D051379:Mice; D008820:Mice, Obese; D008968:Molecular Conformation; D009765:Obesity / Q000188:drug therapy; D051381:Rats; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D019440:Anti-Obesity Agents; D001562:Benzimidazoles; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin