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

L Ma, Z Yang, C Li, Z Zhu, X Shen…

Index: Ma, Lei; Yang, Zhengyi; Li, Chenjing; Zhu, Zhiyuan; Shen, Xu; Hu, Lihong Journal of Enzyme Inhibition and Medicinal Chemistry, 2011 , vol. 26, # 5 p. 643 - 648

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Citation Number: 9

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 ...