Discovery of pyrazolo[3,4-d]pyrimidine derivatives as GPR119 agonists.
Bioorg Med Chem Lett
; 24(3): 949-53, 2014 Feb 01.
Article
en En
| MEDLINE
| ID: mdl-24412066
ABSTRACT
We designed and synthesized a novel series of phenylamino- and phenoxy-substituted pyrazolo[3,4-d]pyrimidine derivatives as GPR119 agonists. SAR studies indicated that electron-withdrawing substituents on the phenyl ring are important for potency and full efficacy. Compound 26 combined good potency with a promising pharmacokinetic profile in mice, and lowered the glucose excursion in mice in an oral glucose-tolerance test.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Pirimidinas
/
Receptores Acoplados a Proteínas G
/
Descubrimiento de Drogas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2014
Tipo del documento:
Article