Author/Authors :
Cédrik Garino، نويسنده , , Nicolas Pietrancosta، نويسنده , , Younes Laras، نويسنده , , Vincent Moret، نويسنده , , Amandine Rolland، نويسنده , , Gilles Quéléver، نويسنده , , Jean-Louis Kraus، نويسنده ,
Abstract :
The protease β-secretase plays a central role in the synthesis of pathogenic amyloid-β in Alzheimer’s disease. Here, we report a new series of analogues based on the phenyl-piperazine scaffold coupled to various heterocyclic moieties, which demonstrate improved inhibitory activities on BACE-1 (FRET assay) compared to already known naphthyl counterparts. The obtained results suggest further structural modifications to access to more potent BACE-1 inhibitors.
