Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.

Abstract The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100 nM. Compounds 19 and 28 , two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.