In this study, we report the synthesis of thiazole Schiff base derivatives (Z1-Z16) and their tyrosinase inhibitory activity, anti-oxidant activities. Mushroom tyrosinase inhibitory assay showed compound Z8 (IC50 = 2.78 ± 0.08 μM) inhibited tyrosinase more than kojic acid (49.39 ± 0.17 μM), and docking study indicated compound Z8 (-7.32 kcal/mol) had stronger binding affinities for tyrosinase than kojic acid (-5.7 kcal/mol). Phenolic hydroxyl group on 4-position (R2) of compound Z8 can form Metal - Acceptor with Cu401. The results of inhibition kinetics studies demonstrated that compound Z8 was mixed type inhibitor. The anti-browning effects manifested compound Z8 expressed satisfactory effects in anti-browning of fresh-cut apples and fresh-cut potato. All the results indicated that thiazole Schiff base derivatives might be promising leading compounds as tyrosinase inhibitors and anti-oxidant agents.

中文翻译：

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噻唑席夫碱衍生物的生物学评价与合成

在这项研究中，我们报告了噻唑席夫碱衍生物 ( Z1 - Z16 )的合成及其酪氨酸酶抑制活性、抗氧化活性。蘑菇酪氨酸酶抑制试验表明，化合物Z8 (IC 50 = 2.78 ± 0.08 μM) 对酪氨酸酶的抑制作用大于曲酸 (49.39 ± 0.17 μM)，对接研究表明化合物Z8 (-7.32 kcal/mol) 对酪氨酸酶的结合亲和力强于酪氨酸酶酸（-5.7 kcal/mol）。化合物Z8的4位(R 2 )上的酚羟基可与Cu4O1形成金属-受体。抑制动力学研究结果表明，化合物Z8是混合型抑制剂。抗褐变效果表明化合物Z8在鲜切苹果和鲜切马铃薯的抗褐变方面表现出令人满意的效果。所有结果表明，噻唑席夫碱衍生物可能是作为酪氨酸酶抑制剂和抗氧化剂的有前途的领先化合物。