目的 设计合成一系列熊果苷类似物,并评价其酪氨酸酶抑制活性.方法 以邻苯二酚、间苯二酚、对苯二酚为原料,通过一侧酚羟基的苄基保护,与溴乙酰基半乳糖、葡萄糖、木糖、阿拉伯糖进行偶联并脱除保护基,得到11个未见报道的熊果苷类似物.通过1 H-NMR、”C-NMR、HRMS等波谱分析方法对所合成的11个目标化合物进行结构表征.以α-熊果苷为阳性对照,对目标化合物及中间体进行抗酪氨酸酶活性测试.结果与结论 目标化合物具有良好的酪氨酸酶抑制活性.其中,化合物p-5a、o-5a、p-4d、m-4d、m-5d的活性与阳性对照物α-熊果苷相当,化合物p-5d的活性优于阳性对照物α-熊果苷.“,”A series of arbutin analogues were designed and synthesized.Three kinds of hydroquinones with mono-protection of phenolic hydroxyl group were directly coupled with bromoacetylgalactose,glucose,xylose and arabinose,then removed the protecting groups to get eleven target compounds.The target compounds were characterized by 1H-NMR,13C-NMR and HRMS.The results of whitening activity of these analogues indicated p-5a,o-5a,p-4d,m-4d and m-5d had significant inhibition against tyrosinase,and the inhibition activity of p-5d against tyrosinase was obviously better than that of positive control α-arbutin.