BACE-1 inhibitors part 2: Identification of hydroxy ethylamines (HEAs) with reduced peptidic character

Modification of the prime side of a lead di-amide series of BACE-1 inhibitors was investigated. Inhibitors with reduced peptidic character are presented and two different enzyme-binding modes are described. The compounds described lower amyloid production in a cell-based assay at sub-micromolar concentrations.