1.
Bioorg Med Chem Lett
; 21(1): 497-501, 2011 Jan 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21075628
RESUMEN
The discovery and structure-activity relationship of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB(1) receptor is disclosed. Compound 26i was found to be a high potency, selective cannabinoid CB(1) antagonist.
Asunto(s)
Amidas/química , Indoles/química , Receptor Cannabinoide CB1/antagonistas & inhibidores , Amidas/síntesis química , Amidas/farmacocinética , Animales , Perros , Evaluación Preclínica de Medicamentos , Indoles/síntesis química , Indoles/farmacocinética , Masculino , Ratones , Modelos Moleculares , Ratas , Ratas Wistar , Receptor Cannabinoide CB1/metabolismo , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 15(3): 589-93, 2005 Feb 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-15664818
RESUMEN
A series of 3-phenoxypropyl piperidine analogues have been discovered as novel ORL1 receptor agonists. Structure-activity relationships have been explored around the 3-phenoxypropyl region with several potent and selective analogues identified.