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学科主题: 生命有机化学
题名: 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
作者: Wang DY(王东业) ; Wu YL(吴毓林) ; Wu YK(伍贻康) ; Liang J(梁杰) ; Li Y(李英)
通讯作者: 吴毓林
刊名: J. Chem. Soc.-Perkin Trans. 1
发表日期: 2001
期: 6, 页:605-609
收录类别: SCI
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
英文摘要: 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.
语种: 英语
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WOS记录号: WOS:000167727700006
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/13998
Appears in Collections:生命有机化学国家重点实验室_期刊论文

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Recommended Citation:
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.
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