Tetrahydroisoquinolines as MCH-R1 antagonists.
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.
Sasikumar
T K
TK
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. thavalakulamgar.sasikumar@spcorp.com
Qiang
L
L
Wu
W-L
WL
Burnett
D A
DA
Greenlee
W J
WJ
O'Neill
K
K
Hawes
B E
BE
van Heek
M
M
Graziano
M
M
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*
D001562:Benzimidazoles; C103263:MCHR1 protein, human; C491208:MCHR1 protein, rat; D017481:Receptors, Somatostatin; D044005:Tetrahydroisoquinolines; C031000:benzimidazole