Bioorganic and Medicinal Chemistry Letters p. 1146 - 1150 (2008)
Update date:2022-08-04
Topics:
Li, Guoqing
Stamford, Andrew W.
Huang, Ying
Cheng, Kuo-Chi
Cook, John
Farley, Constance
Gao, Jun
Ghibaudi, Lorraine
Greenlee, William J.
Guzzi, Mario
van Heek, Margaret
Hwa, Joyce J.
Kelly, Joe
Mullins, Deborra
Parker, Eric M.
Wainhaus, Sam
Zhang, Xiaoping
We have derived a novel series of neuropeptide Y (NPY) Y5 receptor antagonists from the biphenylurea 3. Cyclohexylurea 21c, a member of the series, is a potent NPY Y5 receptor antagonist that exhibits excellent pharmacokinetic parameters in rats and dogs. On chronic oral administration to diet-induced obese rats, 21c displayed an anti-obesity profile, causing a modest reduction in food intake, a significant decrease in body weight gain, a decrease in adipose mass, and an increase in lean tissue mass.
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