Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists.

Design, synthesis, structure–activity relationship, and in vivo pharmacological data of a series of 3H-spiro[isobenzofuran-1,4’-piperidine] based compounds as potent, selective, orally bioavailable and brain penetrable melanocortin subtype-4 receptor (MC4R) agonists are disclosed.