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.
MeSH terms
-
Animals
-
Benzimidazoles / chemistry
-
Humans
-
Molecular Structure
-
Rats
-
Receptors, Somatostatin / antagonists & inhibitors*
-
Receptors, Somatostatin / metabolism
-
Structure-Activity Relationship
-
Tetrahydroisoquinolines / chemical synthesis*
-
Tetrahydroisoquinolines / chemistry
-
Tetrahydroisoquinolines / pharmacokinetics
-
Tetrahydroisoquinolines / pharmacology*
Substances
-
Benzimidazoles
-
MCHR1 protein, human
-
MCHR1 protein, rat
-
Receptors, Somatostatin
-
Tetrahydroisoquinolines
-
benzimidazole