1.
Bioorg Med Chem Lett
; 15(23): 5293-7, 2005 Dec 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16203136
RESUMEN
The synthesis and biological evaluation of novel 3-amino indazole melanin concentrating hormone receptor-1 antagonists are reported, several of which demonstrated functional activity of less than 100nM. Compounds 19 and 28, two of the more potent compounds identified in this study, were characterized by high exposure in the brain and demonstrated robust efficacy when dosed in diet-induced obese mice.
Asunto(s)
Fármacos Antiobesidad/síntesis química , Fármacos Antiobesidad/farmacología , Indazoles/síntesis química , Indazoles/farmacología , Receptores de Somatostatina/antagonistas & inhibidores , Administración Oral , Animales , Fármacos Antiobesidad/administración & dosificación , Humanos , Indazoles/administración & dosificación , Ratones , Piperidinas/química , Distribución Tisular
2.
Bioorg Med Chem Lett
; 15(19): 4174-9, 2005 Oct 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-16085414
RESUMEN
Several potent and efficacious MCHr1 antagonists containing an ortho-amino benzamide or nicotinamide chemotype have been identified, exemplified by 28 and 50.
