Preparation of ferulic acid derivatives and evaluation of their xanthine oxidase inhibition activity |
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Authors: | Wang Feng Yang Leixiang Huang Kexin Li Xiaokun Hao Xiaojiang Stöckigt Joachim Zhao Yu |
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Institution: | Department of Traditional Chinese Medicine and Natural Drug Research, College of Pharmaceutical Sciences, Zhejiang University, 353 Yan An Road, Hangzhou 310031, China. |
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Abstract: | Several ferulic acid ethyl esters (3a-h) were synthesized under the Knoevengel reaction condition and they were further reduced to afford the respective allylic alcohol derivatives (4a-g). Some of them were evaluated for the xanthine oxidase (XO) inhibitory activity. Among them, 3h exhibited a significant inhibitory activity with an IC50 value of 1.35 x 10(-5) M, while the IC50 value of allopurinol used as the positive control was 1.49 x 10(-5) M. The study suggested that the higher acidity of the phenolic OH group in the ferulic acid derivatives might result in improved XO inhibitory activity. |
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