1.
J Med Chem
; 51(13): 3946-52, 2008 Jul 10.
Artículo
en Inglés
| MEDLINE
| ID: mdl-18553956
RESUMEN
Selective bradykinin (BK) B 1 receptor antagonists could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure activity relationships of the structurally novel HTS lead compound 1 provided potent hBK B 1 receptor antagonists with excellent receptor occupancy in the CNS of hBK B 1 transgenic rats.
Asunto(s)
Aminas/química , Benzofenonas/química , Benzofenonas/farmacología , Antagonistas del Receptor de Bradiquinina B1 , Animales , Benzofenonas/síntesis química , Línea Celular , Perros , Humanos , Estructura Molecular , Ratas , Receptor de Bradiquinina B1/metabolismo , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 17(11): 3006-9, 2007 Jun 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-17428657
RESUMEN
Selective bradykinin (BK) B(1) receptor antagonists have been shown to be antinociceptive in animal models and could be novel therapeutic agents for the treatment of pain and inflammation. Elucidation of the structure-activity relationships of the biphenyl moiety of the lead compound 1 provided a potent new structural class of BK B(1) receptor antagonists.
