1.
Bioorg Med Chem Lett
; 12(13): 1755-8, 2002 Jul 08.
Artículo
en Inglés
| MEDLINE
| ID: mdl-12067554
RESUMEN
A series of novel 4,4-disubstituted cyclohexylamine based NK(1) antagonists is described. The effect of changes to the C(1)-C(4) relative stereochemistry on the cyclohexane ring and replacements for the flexible linker are discussed, leading to the identification of compounds with high affinity and good in vivo duration of action.
Asunto(s)
Ciclohexilaminas/síntesis química , Ciclohexilaminas/farmacología , Antagonistas del Receptor de Neuroquinina-1 , Animales , Sitios de Unión , Células CHO , Sistema Nervioso Central/efectos de los fármacos , Sistema Nervioso Central/metabolismo , Cricetinae , Ciclohexilaminas/farmacocinética , Gerbillinae , Concentración 50 Inhibidora , Conformación Molecular , Ensayo de Unión Radioligante , Receptores de Neuroquinina-1/química , Relación Estructura-Actividad
2.
Bioorg Med Chem Lett
; 12(13): 1759-62, 2002 Jul 08.
Artículo
en Inglés
| MEDLINE
| ID: mdl-12067555
RESUMEN
A series of novel 4,4-disubstituted cyclohexylamines as NK(1) receptor antagonists is described: modifications to the amine moiety retain NK(1) receptor binding affinity whilst disrupting I(Kr) affinity.
