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ID: ALA1143109
Journal: Bioorg Med Chem Lett
Title: Discovery of novel orally active ureido NPY Y5 receptor antagonists.
Authors: Li G, Stamford AW, Huang Y, Cheng KC, Cook J, Farley C, Gao J, Ghibaudi L, Greenlee WJ, Guzzi M, van Heek M, Hwa JJ, Kelly J, Mullins D, Parker EM, Wainhaus S, Zhang X.
Abstract: 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.
CiteXplore: 18160282