| 16412632 |
Garino C, Pietrancosta N, Laras Y, Moret V, Rolland A, Quelever G, Kraus JL: BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1995-9. Epub 2006 Jan 18.
The protease beta-secretase plays a central role in the synthesis of pathogenic amyloid-beta 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. |
164(2,2,2,4) |