| 抗日本血吸虫病药物研究——Ⅱ.溴乙酸及碘乙酸香豆素酯的合成 |
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| 引用本文： | 王锐,应慧卿,冷宗康,顾旭初,邹树炯,潘秀华. 抗日本血吸虫病药物研究——Ⅱ.溴乙酸及碘乙酸香豆素酯的合成[J]. 药学学报, 1981, 16(10): 779-783 |
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| 作者姓名： | 王锐 应慧卿 冷宗康 顾旭初 邹树炯 潘秀华 |
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| 作者单位： | 南京药物研究所(王锐，应慧卿，冷宗康，顾旭初，邹树炯)，南京药物研究所(潘秀华) |
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| 摘 要： | 溴乙酸醇酯、酚酯类化合物作为抗日本血吸虫病药物的研究,前已报道。鉴于在筛选中发现4-甲基-7-羟基香豆素的溴乙酸酯具有明显的杀血吸虫作用,而文献报道香豆素衍生物具有广泛的生理活性,因此又合成了一系列羟基香豆素的溴(或碘)乙酸酯类化合物,以
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| 收稿时间： | 1980-05-22 |
STUDIES ON CHEMOTHERAPEUTIC AGENTS AGAINST SCHISTOSOMIASIS JAPONICA Ⅱ. SYNTHESIS OF COUMARIN ESTERS OF MONOBROMO- AND MONOIODOACETIC ACID |
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| Wang Rui,Ying Huiqing,Leng Zongkang,Gu Xuchu,Zou Shujiong and Pan Xiuhua. STUDIES ON CHEMOTHERAPEUTIC AGENTS AGAINST SCHISTOSOMIASIS JAPONICA Ⅱ. SYNTHESIS OF COUMARIN ESTERS OF MONOBROMO- AND MONOIODOACETIC ACID[J]. Acta pharmaceutica Sinica, 1981, 16(10): 779-783 |
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| Authors: | Wang Rui Ying Huiqing Leng Zongkang Gu Xuchu Zou Shujiong Pan Xiuhua |
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| Abstract: | In a preceding paper of this series, we reported the synthesis of alcoholic and phenolic esters of monobromo- and monoiodoacetic acid which were found to possess schistosomicidal activity both in mice and in dogs. In order to search for more active schistosomicidal drugs, twenty-two coumarin esters of monobromo-and monoiodoacetic acid were prepared and tested for schistosomicidal activity. In screening with mice, 21 compounds were found to possess schistosomicidal activity, among which 3-(2'-bromoacetoxy ) coumarin and 4-methyl- 6,7-bis- (2'-bromoacetoxy) coumarin were shown to be the most effective and their worm reduction rates reached 100%. |
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