Institute of Organic Chemistry, School of Chemistry and Chemical Engineering, Sun Yat-sen University, PR China.
Bioorg Med Chem. 2011 Feb 1;19(3):1167-71. doi: 10.1016/j.bmc.2010.12.051. Epub 2010 Dec 30.
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 IC(50) less than 10μM. Further studies showed these five compounds were competitive inhibitors of tyrosinase and their structure-activity relationships were investigated in this article.
在我们的研究中，合成了 14 种带有羟基的苄基苯甲酸酯（3-16），并测试了它们对蘑菇酪氨酸酶的抑制活性。结果表明，在这些化合物中，4-羟基苄基 3,5-二羟基苯甲酸酯（3）、4-羟基苄基 2,4-二羟基苯甲酸酯（5）、4-羟基苄基 2,4,6-三羟基苯甲酸酯（7）、3-羟基苄基 3,5-二羟基苯甲酸酯（8）、3-羟基苄基 2,4-二羟基苯甲酸酯（10）具有抑制活性，其 IC50 均小于 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。
