Identification of piperazine-bisamide GHSR antagonists for the treatment of obesity.
Bioorg Med Chem Lett
; 20(5): 1758-62, 2010 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-20137933
ABSTRACT
Piperazine-bisamide analogs were discovered as partial agonists of human growth hormone secretagogue receptor (GHSR) in a high throughput screen. The partial agonists were optimized for potency and converted into antagonists through structure-activity relationship (SAR) studies. The efforts also led to the identification of potent antagonist with favorable PK profile suitable as a tool compound for in vivo studies.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Fármacos Antiobesidade
/
Receptores de Grelina
/
Amidas
/
Indóis
Tipo de estudo:
Diagnostic_studies
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Ano de publicação:
2010
Tipo de documento:
Article