Discovery of novel orally active ureido NPY Y5 receptor antagonists.
Bioorg Med Chem Lett
; 18(3): 1146-50, 2008 Feb 01.
Article
in En
| MEDLINE
| ID: mdl-18160282
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.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Urea
/
Receptors, Neuropeptide Y
/
Anti-Obesity Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2008
Document type:
Article
Affiliation country:
United States
Publication country:
ENGLAND
/
ESCOCIA
/
GB
/
GREAT BRITAIN
/
INGLATERRA
/
REINO UNIDO
/
SCOTLAND
/
UK
/
UNITED KINGDOM