Evaluation of dihydropyrimidin-(2H)-one analogues and rhodanine derivatives as tyrosinase inhibitors |
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| Authors: | Liu Jinbing Wu Fengyan Chen Lingjuan Hu Jianming Zhao Liangzhong Chen Changhong Peng Liwang |
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| Institution: | a Department of Biology and Chemical Engineering, Shaoyang University, Shao Shui Xi Road, Shaoyang 422100, People’s Republic of China
b College of Food Science and Engineering, Central South University of Forestry and Technology, People’s Republic of China |
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| Abstract: | A series of dihydropyrimidin-(2H)-one analogues and rhodanine derivatives were synthesized and their inhibitory effects on the diphenolase activity of mushroom tyrosinase were evaluated. The results showed that some of the synthesized compounds exhibited significant inhibitory activities. Especially, compound 15 bearing a hydroxyethoxyl group at position-4 of phenyl ring exhibited most potent tyrosinase inhibitory activity with IC50 value of 0.56 mM. The inhibition mechanism analysis of compound 15 demonstrated that the inhibitory effect of the compound on the tyrosinase was irreversible. These results suggested that such compounds might be served as lead compounds for further designing new potential tyrosinase inhibitors. |
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| Keywords: | Dihydropyrimidin-(2H)-one Rhodanine Tyrosinase inhibitors Inhibition mechanism |
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