In this work, 11 novel compounds based on vaniline and benzylidenehydrazine structure were synthesized with various substituents on phenyl aromatic ring of the molecule and evaluated as tyrosinase inhibitors. These new derivatives showed significant anti-tyrosinase activities, among which 4i demonstrated to be the most potent compound, with IC50 values of 1.58 µM . The structure–activity relationship study of the novel constructed analogs was fully discussed. Kinetic study of compound 4i showed uncompetitive inhibition towards tyrosinase. Furthermore, the high potency of 4i was supported theoretically by molecular docking evaluations.

中文翻译：

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瓦力灵-苄叉肼杂种作为有效酪氨酸酶抑制剂的合成，生物学评估和分子对接分析

在这项工作中，合成了11种基于香草碱和苄叉肼结构的新型化合物，该化合物在分子的苯基芳环上带有多个取代基，并被评估为酪氨酸酶抑制剂。这些新的衍生物显示出显着的抗酪氨酸酶活性，其中4i被证明是最有效的化合物，IC50值为1.58 µM。全面讨论了新型结构类似物的构效关系研究。化合物4i的动力学研究显示对酪氨酸酶的竞争性抑制。此外，分子对接评估在理论上支持了4i的高效能。