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Bioorg Med Chem Lett. 2008 Feb 1;18(3):1146-50. Epub 2007 Dec 5.

Discovery of novel orally active ureido NPY Y5 receptor antagonists.

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Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road MS 2545, Kenilworth, NJ 07033-0359, USA.


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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