A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation

In this work, we report a rational structure-based approach aimed at the discovery of new 2- aminoimidazoles as b-secretase inhibitors. Taking advantage of a microwave-assisted synthetic protocol, a small library of derivatives was obtained and biologically evaluated. Two compounds showed promising activities in both enzymatic and cellular assays. Moreover, one of them exhibited the capa- bility to cross the bloodebrain barrier as assessed by the parallel arti␣cial membrane permeability assay.