Keto-1,3,4-oxadiazoles as cathepsin K inhibitors.
Bioorg Med Chem Lett
; 16(11): 2909-14, 2006 Jun 01.
Article
en En
| MEDLINE
| ID: mdl-16546382
ABSTRACT
We have prepared a series of cathepsin K inhibitors bearing the keto-1,3,4-oxadiazole warhead capable of forming a hemithioketal complex with the target enzyme. By modifying binding moieties at the P1, P2, and prime side positions of the inhibitors, we have achieved selectivity over cathepsins B, L, and S, and have achieved sub-nanomolar potency against cathepsin K. This series thus represents a promising chemotype that could be used in diseases implicated by imbalances in cathepsin K activity such as osteoporosis.
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Banco de datos:
MEDLINE
Asunto principal:
Oxadiazoles
/
Inhibidores de Proteasas
/
Catepsinas
Límite:
Animals
Idioma:
En
Año:
2006
Tipo del documento:
Article