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

Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4′-piperidine] based compounds as potent, selective and orally bioavailable melanocortin subtype-4 receptor (MC4R) agonists are disclosed.

Graphical abstractDesign, 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.Figure optionsDownload full-size imageDownload as PowerPoint slide