1.
Bioorg Med Chem Lett
; 14(16): 4161-4, 2004 Aug 16.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15261262
RESUMEN
Modification of lead compound 1 by reducing lipophilicity in the P3 group produced a series of low molecular weight thrombin inhibitors with excellent potency in functional assays, metabolic stability, and oral bioavailability. These modifications led to the identification of two optimized compounds, 14 and 16.
Asunto(s)
Antitrombinas/farmacología , Administración Oral , Antitrombinas/administración & dosificación , Antitrombinas/farmacocinética , Disponibilidad Biológica , Estabilidad de Medicamentos , Peso Molecular
2.
Bioorg Med Chem Lett
; 13(20): 3477-82, 2003 Oct 20.
Artículo
en Inglés
| MEDLINE
| ID: mdl-14505652
RESUMEN
Thrombin inhibitors incorporating o-aminoalkylbenzylamides in the P1 position were designed, synthesized and found to have enhanced potency and selectivity in several different structural classes. X-ray crystallographic analysis of compound 24 bound in the alpha-thrombin-hirugen complex provides an explanation for these unanticipated results.
