title: Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.
abstract: 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.
authors.affiliation: Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. thavalakulamgar.sasikumar@spcorp.com
authors.forename: T K
authors.initials: TK
authors.lastname: Sasikumar
authors.forename: Li
authors.initials: L
authors.lastname: Qiang
authors.forename: Duane A
authors.initials: DA
authors.lastname: Burnett
authors.forename: William J
authors.initials: WJ
authors.lastname: Greenlee
authors.forename: Brian E
authors.initials: BE
authors.lastname: Hawes
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Kowalski
authors.forename: Kim
authors.initials: K
authors.lastname: O'Neill
authors.forename: Brian D
authors.initials: BD
authors.lastname: Spar
authors.forename: Blair
authors.initials: B
authors.lastname: Weig
mesh_terms: 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
chemical_list: D019440:Anti-Obesity Agents; D001562:Benzimidazoles; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin