Synthesis and SAR of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones as MCH-1 antagonists for the treatment of obesity

✍ Scribed by Mark Hadden; Dustin M. Deering; Alan J. Henderson; Matthew D. Surman; Michele Luche; Yuri Khmelnitsky; Steven Vickers; Jean Viggers; Sharon Cheetham; Peter R. Guzzo

• Book ID: 104004889
• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 645 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.09.037

✦ Synopsis

A new series of 4-aryl-1-(indazol-5-yl)pyridin-2(1H)ones possessing MCH-1 receptor antagonism is presented. Suzuki coupling of boronic acids with key triflate 6 allowed rapid generation of a range of analogs. The SAR of the MCH-1 receptor was explored with a variety of aryl and heterocyclic moieties. Selected compounds were studied in a five-day diet induced obese mouse model to evaluate their potential use as weight loss agents.