Discovery of Bicycloalkyl Urea Melanin Concentrating Hormone Receptor Antagonists:  Orally Efficacious Antiobesity Therapeutics

Abstract

Melanin concentrating hormone (MCH) is involved in regulation of food intake and energy homeostasis. Antagonists of the MCH receptor are expected to affect food intake and weight gain, making MCH-R1 an attractive target for obesity treatment. Herein, we report the discovery of a novel, orally active series of MCH-R1 antagonists that exhibit in vivo efficacy in rodent obesity models.