期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 8, 页码 2376-2379出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.02.076
关键词
Dihydropyrimidin-(2H)-one; Rhodanine; Tyrosinase inhibitors; Inhibition mechanism
资金
- Foundation of Education Department of Hunan Province, China [09B091]
- Key Subject Foundation of Shaoyang University [2008XK201]
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. (C) 2011 Elsevier Ltd. All rights reserved.
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