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Further evidence for the participation of primary carbon-centered free radicals in the antimalarial action of the qinghaosu (artemisinin) series of compounds
其他题名碳自由基参与青蒿素系列化合物的抗虐作用的进一步证据
Wang DY(王东业); Wu YL(吴毓林); Wu YK(伍贻康); Liang J(梁杰); Li Y(李英)
2001
发表期刊J. Chem. Soc.-Perkin Trans. 1
ISSN1472-7781
期号6页码:605-609
摘要Friedel-crafts alkylation of 1,3-dimethoxybenzene with O-acetyldihydroqinghaosu gave a pair of 11-epimers of 12-(2,4-dimethoxyphenyl)deoxoqinghaosu 2 and 2'. The antimalarial activity of 11 β-epimer 2 was comparable with that of artemether. Compound 2 reacted smoothly with ferrous ions or L-cysteine and catalytic amounts of ferrous ions to give a series of products derived from the previously postulated C-centered free radical, in particular the primary C-centered free radical. However, 11α-epimer 2'was almost inert to ferrous ions and also showed low antimalarial activity. The identification of free radical mediated products and the correlation between chemical reactivity and bio-activity once again provided evidence for the key role of primary carbon-centered free radicals in the antimalarial activity of the qinghaosu seres of compounds.
学科领域生命有机化学
部门归属中国科学院上海有机化学研究所生命有机化学实验室; 上海药物所
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收录类别SCI
语种英语
WOS记录号WOS:000167727700006
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被引频次:24[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.sioc.ac.cn/handle/331003/13998
专题生命有机化学国家重点实验室
通讯作者Wu YL(吴毓林)
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GB/T 7714
Wang DY,Wu YL,Wu YK,et al. Further evidence for the participation of primary carbon-centered free radicals in the antimalarial action of the qinghaosu (artemisinin) series of compounds[J]. J. Chem. Soc.-Perkin Trans. 1,2001(6):605-609.
APA 王东业,吴毓林,伍贻康,梁杰,&李英.(2001).Further evidence for the participation of primary carbon-centered free radicals in the antimalarial action of the qinghaosu (artemisinin) series of compounds.J. Chem. Soc.-Perkin Trans. 1(6),605-609.
MLA 王东业,et al."Further evidence for the participation of primary carbon-centered free radicals in the antimalarial action of the qinghaosu (artemisinin) series of compounds".J. Chem. Soc.-Perkin Trans. 1 .6(2001):605-609.
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