Department of Biology and Chemical Engineering, Shaoyang University, Shao Shui Xi Road, Shaoyang 422100, PR China.
Food Chem. 2012 Dec 15;135(4):2872-8. doi: 10.1016/j.foodchem.2012.07.055. Epub 2012 Jul 24.
A series of coumarin derivatives were synthesised and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were evaluated. The results showed that some of the synthesised compounds exhibited significant inhibitory activities. Especially, 2-(1-(coumarin-3-yl)ethylidene)hydrazinecarbothioamide bearing thiose-micarbazide group exhibited the most potent tyrosinase inhibitory activity with IC(50) value of 3.44μM. The inhibition mechanism analysis of 2-(1-(coumarin-3-yl)-ethylidene)hydrazinecarbothioamide and 2-(1-(6-chlorocoumarin-3-yl)ethylidene)-hydrazinecarbothioamide demonstrated that the inhibitory effects of the compounds on the tyrosinase were irreversible. Preliminary structure activity relationships' (SARs) analysis suggested that further development of such compounds might be of interest.
一系列香豆素衍生物被合成，并评估了它们对蘑菇酪氨酸酶二酚酶活性的抑制作用。结果表明，一些合成的化合物表现出显著的抑制活性。特别是含有噻唑-氨基甲脒基团的 2-(1-(香豆素-3-基)亚乙基)肼二硫代甲酰胺表现出最强的酪氨酸酶抑制活性，IC50值为 3.44μM。对 2-(1-(香豆素-3-基)-亚乙基)肼二硫代甲酰胺和 2-(1-(6-氯香豆素-3-基)亚乙基)肼二硫代甲酰胺的抑制机制分析表明，这些化合物对酪氨酸酶的抑制作用是不可逆的。初步的构效关系（SARs）分析表明，进一步开发此类化合物可能具有一定的研究价值。
