Design and synthesis of cyclic acylguanidines as BACE1 inhibitors

Based on the lead compound 1 reported in literature, a series of novel BACE1 inhibitors were designed and synthesized, among which compound 11 exhibited a 14-fold improvement in potency over the lead compound 1. This represents a good lead for the discovery of more promising BACE1 inhibitors for the potential treatment of AD.

Graphical abstractCompounds with much improved BACE1 inhibitory potency than the lead compound 1 were obtained.Figure optionsDownload full-size imageDownload as PowerPoint slide