BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.

Modifications to the non-prime side of a series of BACE-1 inhibitors are presented. This final round of optimisation led to inhibitors with nanomolar potency in a cell-based assay which were capable of lowering amyloid production in an animal model following oral administration.