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.
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.
Wang Rui, Ying Huiqing, Leng Zongkang, Gu Xuchu, Zou Shujiong , Pan Xiuhua, . STUDIES ON CHEMOTHERAPEUTIC AGENTS AGAINST SCHISTOSOMIASIS JAPONICA Ⅱ. SYNTHESIS OF COUMARIN ESTERS OF MONOBROMO- AND MONOIODOACETIC ACIDJ. Acta Pharmaceutica Sinica, 1981, 16(10): 779-783.
Citation: Wang Rui, Ying Huiqing, Leng Zongkang, Gu Xuchu, Zou Shujiong , Pan Xiuhua, . STUDIES ON CHEMOTHERAPEUTIC AGENTS AGAINST SCHISTOSOMIASIS JAPONICA Ⅱ. SYNTHESIS OF COUMARIN ESTERS OF MONOBROMO- AND MONOIODOACETIC ACIDJ. Acta Pharmaceutica Sinica, 1981, 16(10): 779-783.

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

STUDIES ON CHEMOTHERAPEUTIC AGENTS AGAINST SCHISTOSOMIASIS JAPONICA Ⅱ. SYNTHESIS OF COUMARIN ESTERS OF MONOBROMO- AND MONOIODOACETIC ACID

  • 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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