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本文合成了一系列卤代查尔酮及其氨基硫脲席夫碱,并考察了所合成化合物的酪氨酸酶抑制活性及抗氧化活性。结果表明,部分化合物具有较好的酪氨酸酶抑制活性,其中3个化合物的抑制活性强于阳性对照曲酸,4-溴代查尔酮氨基硫脲席夫碱(化合物9)表现出最好的抑制活性,其IC50值为2.02μmol/L;部分化合物还具有一定的抗氧化活性。抑制机理研究表明,化合物9属于不可逆抑制剂。优选化合物9进行了分子对接探讨,初步构效关系分析为进一步研究具有酪氨酸酶抑制活性的类似化合物提供了参考。
In this paper, a series of halogenated Chalcones and their thiosemicarbazones were synthesized and the tyrosinase inhibitory activity and antioxidant activity of the synthesized compounds were investigated. The results showed that some of the compounds showed good tyrosinase inhibitory activity. Among them, the inhibitory activity of three compounds was stronger than that of the positive control kojic acid, and the 4-bromochlorone thiosemicarbazone Schiff base (compound 9) Good inhibitory activity, the IC50 value of 2.02μmol / L; some compounds also have some antioxidant activity. Inhibition mechanism studies show that compound 9 is an irreversible inhibitor. The optimal compound 9 has been studied by molecular docking. The preliminary structure-activity relationship analysis provides a reference for further research on similar compounds with tyrosinase inhibitory activity.