Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.
Bioorg Med Chem Lett
; 22(12): 3890-4, 2012 Jun 15.
Article
em En
| MEDLINE
| ID: mdl-22617492
ABSTRACT
A series of orexin receptor antagonists was synthesized based on a substituted piperidine scaffold. Through traditional medicinal chemistry structure-activity relationships (SAR), installation of various groups at the 3-6-positions of the piperidine led to modest enhancement in receptor selectivity. Compounds were profiled in vivo for plasma and brain levels in order to identify candidates suitable for efficacy in a model of drug addiction.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Antipsicóticos
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Receptores de Neuropeptídeos
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Receptores Acoplados a Proteínas G
Limite:
Animals
/
Humans
Idioma:
En
Ano de publicação:
2012
Tipo de documento:
Article