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Alternative TitleSynthesis and activity on tyrosinase of novel chalcone derivatives
牛超; 李根; 买迪娜; 阿吉艾克拜尔·艾萨
Source Publication高等学校化学学报

合成了8个新型含苯并噻唑环的查尔酮衍生物及8个酰胺查尔酮,并对化合物的结构进行了表征. 生物活性测试结果表明,化合物4d,4h,5d,7b 和7d 表现出一定的酪氨酸酶激动活性,其中化合物7d 对酪氨酸酶的活性最好,其EC_(50) = 9. 6 mumol /L,优于阳性对照药8-MOP(EC_(50) = 14. 8 mumol /L).

Other Abstract

Ver-nohia anthelmintica L was endemic plant in Xinjiang, which was often used in the treatment of Vitiligo. It was believed that the chalcone compounds of Ver-nohia anthelmintica L played an important role in this treatment. Since it may activate tyrosinase and improve the melanin production, many chalcone compounds and derivatives were described as potential inhibitor on tyrosinase which may act as skin lightening and whitening agents. However, chalcones which showed activator effect were seldom reported. In order to search for chalcones with high activities on tyrosinase, eight novel chalcone derivatives containing benzothiazole and eight amide-derived chalcones were synthesized in this work. All the compounds were identified by 1H NMR, 13C NMR, IR, HRMS and evaluated their activator effect on tyrosinase by measuring the oxidation rate of L-dopa. Compared with the reference drug 8-methoxypsoralen, compounds 4d, 4h, 5d, 7b and 7d showed some activator effect on tyrosinase. Amomg them, compound 7d demonstrated more potent activity with EC50=9.6 μmol/L than 8-methoxypsoralen, which EC50 value was 14.8 μmol/L. Further structural modification of this novel chalcones containing benzothiazole will be required for improving the solubility of them.

Keyword查尔酮 苯并噻唑 酰胺 酪氨酸酶活性
Indexed BySCI ; CSCD
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Cited Times:1[CSCD]   [CSCD Record]
Document Type期刊论文
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GB/T 7714
牛超,李根,买迪娜,等. 新型查尔酮衍生物的合成及酪氨酸酶活性[J]. 高等学校化学学报,2014,35(6):1204-1211.
APA 牛超,李根,买迪娜,&阿吉艾克拜尔·艾萨.(2014).新型查尔酮衍生物的合成及酪氨酸酶活性.高等学校化学学报,35(6),1204-1211.
MLA 牛超,et al."新型查尔酮衍生物的合成及酪氨酸酶活性".高等学校化学学报 35.6(2014):1204-1211.
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