Benzyl benzoates: New phlorizin analogs as mushroom tyrosinase inhibitors.
Benzyl benzoates: New phlorizin analogs as mushroom tyrosinase inhibitors.
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DOI：
10.1016/j.bmc.2010.12.051
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发表时间：
2011-02
影响因子：
3.5
通讯作者：
Y. Fang;Yaozong Chen;Guanfeng Feng;Lin Ma
中科院分区：
文献类型：
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作者：
Y. Fang;Yaozong Chen;Guanfeng Feng;Lin Ma
在我们的研究中，合成了 14 种带有羟基（3-16）的苯甲酸苄酯，并测试了它们对蘑菇酪氨酸酶的抑制活性。结果表明，这些化合物中，3,5-二羟基苯甲酸4-羟基苯甲酯(3)、2,4-二羟基苯甲酸4-羟基苯甲酯(5)、2,4,6-二羟基苯甲酸4-羟基苯甲酯(7)、3,5-二羟基苯甲酸3-羟基苯甲酯(8)、2,4-二羟基苯甲酸3-羟基苯甲酯(10)表现出抑制活性。 IC50小于10μM。进一步的研究表明这五种化合物是酪氨酸酶的竞争性抑制剂，本文对它们的构效关系进行了研究。
In our research, 14 benzyl benzoates with hydroxyl(s) (3–16) were synthesized and their inhibitory activity on mushroom tyrosinase was tested. Results indicated that among these compounds, 4-hydroxybenzyl 3,5-dihydroxybenzoate (3), 4-hydroxybenzyl 2,4-dihydroxybenzoate (5), 4-hydroxybenzyl 2,4,6-dihydroxybenzoate (7), 3-hydroxybenzyl 3,5-dihydroxybenzoate (8), 3-hydroxybenzyl 2,4-dihydroxybenzoate (10) exhibited inhibitory activity with their IC50less than 10μM. Further studies showed these five compounds were competitive inhibitors of tyrosinase and their structure–activity relationships were investigated in this article.