Discovery of benzimidazole pyrrolidinyl amides as prolylcarboxypeptidase inhibitors.
Bioorg Med Chem Lett
; 21(5): 1299-305, 2011 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-21315588
ABSTRACT
A series of benzimidazole pyrrolidinyl amides containing a piperidinyl group were discovered as novel prolylcarboxypeptidase (PrCP) inhibitors. Low-nanomolar IC(50)'s were achieved for several analogs, of which compound 9b displayed modest ex vivo target engagement in eDIO mouse plasma. Compound 9b was also studied in vivo for its effect on weight loss and food intake in an eDIO mouse model and the results will be discussed.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Pirrolidinas
/
Benzimidazóis
/
Carboxipeptidases
/
Inibidores Enzimáticos
/
Descoberta de Drogas
/
Amidas
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos