The design and synthesis of a tricyclic single-nitrogen scaffold that serves as a 5-HT2C receptor agonist.
Bioorg Med Chem Lett
; 16(15): 4130-4, 2006 Aug 01.
Article
em En
| MEDLINE
| ID: mdl-16750364
ABSTRACT
5-HT2C agonists have shown efficacy in limiting food consumption and thus may serve as an important drug class in combating obesity. We describe the design and synthesis of a novel tricyclic single-nitrogen scaffold that was used to produce 5-HT2C agonists. SAR was developed around this chemotype and compounds were identified that were potent (Ki<15 nM) and selective relative to other 5-HT2 receptors. The most promising compound displayed a good pharmacokinetic profile in multiple animal species, and was efficacious in an acute feeding study in rats.
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Base de dados:
MEDLINE
Assunto principal:
Agonistas do Receptor de Serotonina
/
Agonistas do Receptor 5-HT2 de Serotonina
/
Nitrogênio
Limite:
Animals
Idioma:
En
Ano de publicação:
2006
Tipo de documento:
Article