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

Abstract

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).

Keywords::

• Alzheimer’s disease
• BACE1
• chalcone
• SAR
• Glycyrrhiza uralensis