Document Report Card

ID: ALA1140323

Journal: J Med Chem

Title: Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.

Authors: Palani A, Shapiro S, McBriar MD, Clader JW, Greenlee WJ, Spar B, Kowalski TJ, Farley C, Cook J, van Heek M, Weig B, O'neill K, Graziano M, Hawes B.

Abstract: Herein, we report a small molecule MCH-R1 antagonist which demonstrates oral efficacy in chronic rodent models. Substituted phenyl biaryl urea derivatives were synthesized and evaluated as MCH-R1 antagonists for the treatment of obesity. The structure-activity relationship studies in this series resulted in identification of urea 1 as a potent and selective MCH-R1 antagonist. Compound 1 exhibited oral efficacy in chronic (28 d) rodent models at 3-30 mpk showing significant reduction in food intake and weight gain relative to controls.

CiteXplore: 16033253

DOI: 10.1021/jm0503852