Design, synthesis and SAR study of hydroxychalcone inhibitors of human β-secretase (BACE1)

Article abstract of DOI:10.3109/14756366.2010.543420

According to the structural characteristics of isoliquiritigenin from Glycyrrhiza uralensis, a series of hydroxychalcones has been designed, synthesized and evaluated for their in vitro inhibitory activities of β-secretase (BACE1). Structure-activity relationship study suggested that inhibitory activity against BACE1 was governed to a greater extent by the hydroxyl substituent on A-and B-ring of the chalcone, and the most active compound was substituted with four hydroxyl group (17, IC₅₀=0.27 μM).