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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Inhibitory effects of 5-benzylidene barbiturate derivatives on mushroom tyrosinase and their antibacterial activities.
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Inhibitory effects of 5-benzylidene barbiturate derivatives on mushroom tyrosinase and their antibacterial activities.

机译：5-亚苄基巴比妥酸酯衍生物对蘑菇酪氨酸酶的抑制作用及其抗菌活性。

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摘要

A series of novel 5-benzylidene barbiturate and thiobarbiturate derivatives were synthesized and evaluated as tyrosinase inhibitors and antibacterial agents. The results demonstrated that some compounds had more potent inhibitory activities than the parent compound 4-hydroxybenzaldehyde (IC(50)=1.22 mM). Particularly, compounds 1a and 2a were found to be the most potent inhibitors with IC(50) value of 13.98 microM and 14.49 microM, respectively. The inhibition mechanism study revealed that these compounds were irreversible inhibitors. The circular dichroism spectra indicated that these compounds induced conformational changes of mushroom tyrosinase upon binding. In addition, these compounds exhibited selectively antibacterial activity against Staphylococcus aureus. All these results suggested that further development of such compounds may be of interest.
机译：合成了一系列新颖的5-亚苄基巴比妥酸酯和硫代巴比妥酸酯衍生物，并将其用作酪氨酸酶抑制剂和抗菌剂。结果表明，某些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。特别是，发现化合物1a和2a是最有效的抑制剂，IC（50）值分别为13.98 microM和14.49 microM。抑制机理研究表明，这些化合物是不可逆的抑制剂。圆二色性光谱表明，这些化合物在结合后诱导了蘑菇酪氨酸酶的构象变化。另外，这些化合物对金黄色葡萄球菌显示选择性的抗菌活性。所有这些结果表明，这类化合物的进一步开发可能是令人感兴趣的。

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