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

  • J Enzyme Inhib Med Chem. 2011 Oct;26(5):643-8. doi: 10.3109/14756366.2010.543420.
Lei Ma  1 ,  Zhengyi Yang ,  Chenjing Li ,  Zhiyuan Zhu ,  Xu Shen ,  Lihong Hu
Affiliations
  • 1. Shanghai Research Center for Modernization of Traditional Chinese Medicine, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, P. R. China.
PMID: 21222511 DOI: 10.3109/14756366.2010.543420
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, IC(50) = 0.27 μM).

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