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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and biological evaluation of novel 4-hydroxybenzaldehyde derivatives as tyrosinase inhibitors.
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Synthesis and biological evaluation of novel 4-hydroxybenzaldehyde derivatives as tyrosinase inhibitors.

机译：新型4-羟基苯甲醛衍生物作为酪氨酸酶抑制剂的合成及生物学评价。

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摘要

A series of novel 4-hydroxybenzaldehyde derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were investigated. Most of target compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC(50)=1.22 mM). Interestingly, compound 3c bearing a dimethoxyl phosphate was found to be the most potent inhibitor with IC(50) value of 0.059 mM. The inhibition kinetics analyzed by Lineweaver-Burk plots revealed that compound 3c was a non-competitive inhibitor (K(I)=0.0368 mM). In particular, compound 3c showed no side effects at dose of 1600 mg/kg in mice. These results suggested that such compounds might be served as lead compounds for further designing new potential tyrosinase inhibitors.
机译：合成了一系列新型的4-羟基苯甲醛衍生物，并研究了它们对蘑菇酪氨酸酶双酚酶活性的抑制作用。大多数目标化合物具有比母体化合物4-羟基苯甲醛（IC（50）= 1.22 mM）更强的抑制活性。有趣的是，发现带有磷酸二甲氧基酯的化合物3c是最有效的抑制剂，IC（50）值为0.059 mM。通过Lineweaver-Burk图分析的抑制动力学表明，化合物3c是非竞争性抑制剂（K（I）= 0.0368 mM）。特别地，化合物3c在小鼠中以1600mg / kg的剂量没有显示出副作用。这些结果表明，此类化合物可以用作进一步设计新的潜在酪氨酸酶抑制剂的先导化合物。

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