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
em 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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Compostos de Espiro
/
Fármacos Antiobesidade
/
Receptor Tipo 4 de Melanocortina
/
Amidas
/
Obesidade
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2010
Tipo de documento:
Article