Abstract: Based on the chemical structures of magnolol and honokiol, a series of small molecular derivatives were designed for the treatment of Alzheimer′s disease. Through the Discovery Studio, five compounds( 6a - 6e )exhibited the inhibitory activity against Aβ and Tau proteins in all of the designed compounds. Then the five compounds are chemically synthesized and their biological activities were tested by thioflavin T. The result showed that compound 6a had inhibitory effect on the aggregation of two kinds of target proteins at the concentration of 100 μmol/L, which deserves further research.