1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors: separation of desired cellular activity from undesired tissue accumulation through optimization of basic nitrogen pka.
Bioorg Med Chem Lett
; 21(3): 932-5, 2011 Feb 01.
Article
em En
| MEDLINE
| ID: mdl-21227690
ABSTRACT
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.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Inibidores de Proteases
/
Piridinas
/
Catepsinas
/
Nitrogênio
Limite:
Animals
Idioma:
En
Ano de publicação:
2011
Tipo de documento:
Article