Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity.
Bioorg Med Chem Lett
; 20(15): 4399-405, 2010 Aug 01.
Article
in En
| MEDLINE
| ID: mdl-20598882
ABSTRACT
We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds can afford high potency on MC4R as well as good rodent pharmacokinetic profiles. Compound 1r (MK-0489) demonstrates MC4R mediated reduction of food intake and body weight in mouse models. Compound 1r is efficacious in 14-day diet-induced obese (DIO) rat models.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrrolidines
/
Spiro Compounds
/
Anti-Obesity Agents
/
Receptor, Melanocortin, Type 4
/
Amides
/
Obesity
Limits:
Animals
/
Humans
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2010
Document type:
Article
Affiliation country:
United States