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.
MeSH terms
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Administration, Oral
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Animals
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Anti-Obesity Agents / administration & dosage
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Anti-Obesity Agents / chemical synthesis*
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Anti-Obesity Agents / chemistry
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Anti-Obesity Agents / pharmacology*
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Combinatorial Chemistry Techniques
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Dogs
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Humans
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Mice
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Molecular Structure
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Obesity / chemically induced
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Rats
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Receptors, Neuropeptide Y / antagonists & inhibitors*
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Structure-Activity Relationship
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Urea* / administration & dosage
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Urea* / analogs & derivatives
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Urea* / chemical synthesis
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Urea* / chemistry
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Urea* / pharmacology
Substances
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Anti-Obesity Agents
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Receptors, Neuropeptide Y
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neuropeptide Y5 receptor
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Urea