Discovery of aminoheterocycles as potent and brain penetrant prolylcarboxypeptidase inhibitors.
Bioorg Med Chem Lett
; 22(4): 1727-30, 2012 Feb 15.
Article
en En
| MEDLINE
| ID: mdl-22290078
ABSTRACT
Efforts were dedicated to develop potent and brain penetrant prolylcarboxypeptidase (PrCP) inhibitors by replacing the amide group of original leads 1 and 2 with heterocycles. Aminopyrimidines including compound 32a were identified to display good PrCP inhibitory activity (32a, IC(50)=43 nM) and impressive ability to penetrate brain in mice (brain/plasma ratio 1.4).
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Encéfalo
/
Carboxipeptidasas
/
Inhibidores Enzimáticos
/
Descubrimiento de Drogas
/
Aminas
/
Compuestos Heterocíclicos
Límite:
Animals
Idioma:
En
Año:
2012
Tipo del documento:
Article