title: Tetrahydroisoquinolines as MCH-R1 antagonists.
abstract: A series of potent and selective inhibitors of h-MCH-R1 has been developed based on the piperidine glycineamide compounds I and II. These structurally more rigid tetrahydroisoquinolines (III and IV) showed better pharmacokinetics. The highly potent compounds 12d and 12g displayed excellent rat pk.
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: L
authors.initials: L
authors.lastname: Qiang
authors.forename: W-L
authors.initials: WL
authors.lastname: Wu
authors.forename: D A
authors.initials: DA
authors.lastname: Burnett
authors.forename: W J
authors.initials: WJ
authors.lastname: Greenlee
authors.forename: K
authors.initials: K
authors.lastname: O'Neill
authors.forename: B E
authors.initials: BE
authors.lastname: Hawes
authors.forename: M
authors.initials: M
authors.lastname: van Heek
authors.forename: M
authors.initials: M
authors.lastname: Graziano
mesh_terms: D000818:Animals; D001562:Benzimidazoles / Q000737:chemistry; D006801:Humans; D015394:Molecular Structure; D051381:Rats; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*
chemical_list: D001562:Benzimidazoles; C103263:MCHR1 protein, human; C491208:MCHR1 protein, rat; D017481:Receptors, Somatostatin; D044005:Tetrahydroisoquinolines; C031000:benzimidazole