1.
Bioorg Med Chem Lett
; 17(24): 6910-3, 2007 Dec 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17976987
RESUMEN
Several P4 domain derivatives of the general d-phenylglycinamide-based scaffold (2) were synthesized and evaluated for their ability to bind to the serine protease factor Xa. Some of the more potent compounds were evaluated for their anticoagulant effects in vitro. A select subset containing various P1 indole constructs was further evaluated for their pharmacokinetic properties after oral administration to rats.
Asunto(s)
Antitrombina III/síntesis química , Antitrombina III/farmacología , Glicina/análogos & derivados , Anticoagulantes/síntesis química , Anticoagulantes/química , Anticoagulantes/farmacología , Antitrombina III/química , Cristalografía por Rayos X , Factor Xa/química , Factor Xa/metabolismo , Glicina/síntesis química , Glicina/química , Glicina/farmacología , Humanos , Modelos Moleculares , Estructura Molecular , Unión Proteica , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 17(17): 4832-6, 2007 Sep 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17624775
RESUMEN
SAR about the B-ring of a series of N(2)-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1' and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.
