RESUMEN

Two novel RGDF mimetics were synthesized with the use of 4-(1,2,3,4-tetrahydro-isoquinoline-7-yl)amino-4-oxo-butyric acid as a new surrogate of Arg-Gly motif. The synthesized compounds have demonstrated a high potency to inhibit platelet aggregation in vitro and to block FITC-Fg binding to alphaIIbbeta3 on washed human platelets.

Asunto(s)

Receptores Fibrinógenos/antagonistas & inhibidores , Isoquinolinas , Espectroscopía de Resonancia Magnética , Espectrometría de Masa Bombardeada por Átomos Veloces

RESUMEN

The novel fibrinogen receptor antagonists containing fragments of 7-amino-1,2,3,4-tetrahydroisoquinoline and isophthalic acids were synthesized and successfully tested for their ability to inhibit platelet aggregation in vitro and to block FITC-Fg binding to alpha(IIb)beta(3) on washed human platelets.

Asunto(s)

Ácidos Ftálicos/farmacología , Inhibidores de Agregación Plaquetaria/farmacología , Agregación Plaquetaria/efectos de los fármacos , Receptores Fibrinógenos/antagonistas & inhibidores , Unión Competitiva/efectos de los fármacos , Bioensayo , Evaluación Preclínica de Medicamentos , Humanos , Imitación Molecular , Estructura Molecular , Ácidos Ftálicos/síntesis química , Ácidos Ftálicos/química , Inhibidores de Agregación Plaquetaria/síntesis química , Inhibidores de Agregación Plaquetaria/química , Complejo GPIIb-IIIa de Glicoproteína Plaquetaria/efectos de los fármacos , Unión Proteica/efectos de los fármacos , Estereoisomerismo , Relación Estructura-Actividad