Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.
Bioorg Med Chem Lett
; 23(24): 6825-8, 2013 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-24269480
ABSTRACT
A number of new amine scaffolds with good inhibitory activity in the ADP-induced platelet aggregation assay have been found to be potent antagonists of the P2Y1 receptor. SAR optimization led to the identification of isoindoline 3c and piperidine 4a which showed good in vitro binding and functional activities, as well as improved aqueous solubility. Among them, the piperidine 4a showed the best overall profile with favorable PK parameters.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Urea
/
Receptores Purinérgicos P2Y1
/
Agonistas del Receptor Purinérgico P2Y
/
Aminas
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2013
Tipo del documento:
Article