Abstract
Biaryl urea lead compound 1 was discovered earlier in our MCH antagonist program. Novel benzimidazole analogues with increased chemical stability, devoid of the potential carcinogenic liability associated with a biarylamine moiety, were synthesized and evaluated to be potent MCH R1 antagonists. Two compounds in this series have demonstrated in vivo efficacy in a rodent obesity model.
MeSH terms
-
Administration, Oral
-
Animals
-
Anti-Obesity Agents / chemical synthesis*
-
Anti-Obesity Agents / pharmacology*
-
Benzimidazoles / chemical synthesis*
-
Benzimidazoles / pharmacology*
-
Body Weight / drug effects*
-
Disease Models, Animal
-
Drug Design
-
Rats
-
Receptors, Pituitary Hormone / antagonists & inhibitors*
-
Structure-Activity Relationship
Substances
-
Anti-Obesity Agents
-
Benzimidazoles
-
Receptors, Pituitary Hormone
-
melanin-concentrating hormone receptor