Synthesis and antiplatelet effects of an isoxazole series of glycoprotein IIb/IIIa antagonists.
Bioorg Med Chem Lett
; 8(24): 3499-504, 1998 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-9934460
ABSTRACT
Despite the excellent in vitro potency of a series of benzamide glycoprotein IIb/IIIa antagonists, which have been reported previously, poor in vivo potency in the inhibition of platelet aggregation was observed when the most potent inhibitor XU057 was dosed intravenously to dogs. In this communication, we report that replacement of the benzamide in XU057 with an isoxazolecarboxamide resulted in significant improvement in in vivo potency. More importantly, the analogue XU065 showed an excellent oral antiplatelet effect in dogs.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Inhibidores de Agregación Plaquetaria
/
Complejo GPIIb-IIIa de Glicoproteína Plaquetaria
/
Isoxazoles
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
1998
Tipo del documento:
Article
País de afiliación:
Estados Unidos