862652-52-6Relevant academic research and scientific papers
Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity
Palani, Anandan,Shapiro, Sherry,McBriar, Mark D.,Clader, John W.,Greenlee, William J.,Spar, Brian,Kowalski, Timothy J.,Farley, Constance,Cook, John,Van Heek, Margaret,Weig, Blair,O'Neill, Kim,Graziano, Michael,Hawes, Brian
, p. 4746 - 4749 (2005)
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.
