1.
Bioorg Med Chem Lett
; 21(3): 932-5, 2011 Feb 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21227690
RESUMEN
Based on the theoretical understanding of the in vivo lysosomotropism, by adjusting the pk(a) of basic nitrogen containing cathepsin S inhibitors, a set of compounds with pk(a) 6-8 were identified to have excellent cell based Lip10 activity, yet avoiding undesired sequestration in spleen.
Asunto(s)
Catepsinas/antagonistas & inhibidores , Nitrógeno/química , Inhibidores de Proteasas/química , Piridinas/química , Animales , Catepsinas/metabolismo , Ratones , Inhibidores de Proteasas/síntesis química , Inhibidores de Proteasas/farmacocinética , Piridinas/síntesis química , Piridinas/farmacocinética , Ratas , Ratas Sprague-Dawley
2.
Bioorg Med Chem Lett
; 21(10): 3163-7, 2011 May 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-21458261
RESUMEN
The discovery of a novel series of 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamide antagonists of the vasopressin V(1A) receptor is disclosed. Compounds 47 and 48 were found to be high affinity, selective vasopressin V(1A) antagonists.