1.
Bioorg Med Chem Lett
; 30(15): 127279, 2020 08 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-32527459
RESUMEN
The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select compounds were evaluated in vivo to assess their plasma levels in rat.
Asunto(s)
Descubrimiento de Drogas , Factor IXa/antagonistas & inhibidores , Inhibidores del Factor Xa/farmacología , Pirimidinas/farmacología , Relación Dosis-Respuesta a Droga , Factor IXa/metabolismo , Inhibidores del Factor Xa/síntesis química , Inhibidores del Factor Xa/química , Humanos , Estructura Molecular , Pirimidinas/síntesis química , Pirimidinas/química , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 20(3): 1278-83, 2010 Feb 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-20018510
RESUMEN
The syntheses and SAR investigations of novel CB(1) receptor antagonists based on a 1,2-diaryl piperidine core have been described. Optimization of this core afforded a compound with robust in vivo potency by reducing food intake in a mouse DIO model.