4-Substituted cyclohexyl sulfones as potent, orally active γ-secretase inhibitors

Abstract:

The protease γ-secretase plays a pivotal role in the synthesis of pathogenic amyloid-β in Alzheimer’s disease (AD). Here, we report a further extension to a series of cyclohexyl sulfone-based γ-secretase inhibitors which has allowed the preparation of highly potent compounds which also demonstrate robust Aβ(40) lowering in vivo (e.g., compound 32, MED 1mg/kg p.o. in APP-YAC mice).

Año de publicación:

2006

Keywords:

Fuente:

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