颜闵, 张振, 倪志刚, 于继实, 雷兴翰, 席裕瑞, 徐裕信. 丝虫病化学治疗的研究——5-硝基-2-呋喃乙烯衍生物及其类似物的合成J. 药学学报, 1981, 16(12): 902-913.
引用本文: 颜闵, 张振, 倪志刚, 于继实, 雷兴翰, 席裕瑞, 徐裕信. 丝虫病化学治疗的研究——5-硝基-2-呋喃乙烯衍生物及其类似物的合成J. 药学学报, 1981, 16(12): 902-913.
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Yan Min, Zhang Zhen, Ni Zhigang Yu Jishi, , Lei Xinghan Xi Yurui , Xu Yuxin, . CHEMOTHERAPEUTIC STUDIES OF FILARIASIS——SYNTHESIS OF 5-NITRO-2-FURYL-VINYL DERIVATIVES AND THEIR RELATED COMPOUNDSJ. Acta Pharmaceutica Sinica, 1981, 16(12): 902-913.
Citation: Yan Min, Zhang Zhen, Ni Zhigang Yu Jishi, , Lei Xinghan Xi Yurui , Xu Yuxin, . CHEMOTHERAPEUTIC STUDIES OF FILARIASIS——SYNTHESIS OF 5-NITRO-2-FURYL-VINYL DERIVATIVES AND THEIR RELATED COMPOUNDSJ. Acta Pharmaceutica Sinica, 1981, 16(12): 902-913.
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丝虫病化学治疗的研究——5-硝基-2-呋喃乙烯衍生物及其类似物的合成

CHEMOTHERAPEUTIC STUDIES OF FILARIASIS——SYNTHESIS OF 5-NITRO-2-FURYL-VINYL DERIVATIVES AND THEIR RELATED COMPOUNDS

    摘要
  • 摘要: 为了寻找口服抗丝虫病新药,合成了具有碳碳双键乙烯型和碳氮双键甲亚胺型两类化合物共95个。经感染棉鼠丝虫的棉鼠筛选结果,发现有25个化合物对微丝蚴和/或成虫具有明显的抗虫作用。其中以N-(5-硝基-2-呋喃甲叉)-1-氨基四氢-2(1H)嘧啶酮(Ⅱ7)药理编号M-170对成虫有强烈的杀死作用,且毒性较低,已进入初步临床试验。

     

    Abstract: In searching for new oral filaricides ninety-five compounds have been synthesized, and twenty-five compounds were found to have obvious microfilaricidal and/or macrofilaricidal effects. Among them N-(5-nitro-2-furfurylidene) amino tetrahydro-2(1H) pyrimidinone (Ⅱ7) code number M-170, was found to be the most outstanding, especially as macrofilaricide and has been put into preliminary clinical trial.

     

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