4-substituted cyclohexyl sulfones as potent, orally active gamma-secretase inhibitors.
Bioorg Med Chem Lett
; 16(2): 280-4, 2006 Jan 15.
Article
de En
| MEDLINE
| ID: mdl-16275079
ABSTRACT
The protease gamma-secretase plays a pivotal role in the synthesis of pathogenic amyloid-beta in Alzheimer's disease (AD). Here, we report a further extension to a series of cyclohexyl sulfone-based gamma-secretase inhibitors which has allowed the preparation of highly potent compounds which also demonstrate robust Abeta(40) lowering in vivo (e.g., compound 32, MED 1mg/kg p.o. in APP-YAC mice).
Recherche sur Google
Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Endopeptidases
/
Sulfones
/
Cyclohexanes
/
Antienzymes
Limites:
Animals
Langue:
En
Journal:
Bioorg Med Chem Lett
Sujet du journal:
BIOQUIMICA
/
QUIMICA
Année:
2006
Type de document:
Article
Pays d'affiliation:
Royaume-Uni