| 抗血吸虫病药物吡喹酮类似物2-二硫代甲酸酯的合成 |
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| 引用本文： | 李家声,陈伯毅. 抗血吸虫病药物吡喹酮类似物2-二硫代甲酸酯的合成[J]. 重庆医科大学学报, 1988, 0(4) |
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| 作者姓名： | 李家声 陈伯毅 |
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| 作者单位： | 重庆医科大学化学教研室、血吸虫病研究室(李家声)，重庆医科大学化学教研室、血吸虫病研究室(陈伯毅) |
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| 摘 要： | 为寻找抗血吸虫病新药,对吡喹酮的化学结构进行修饰,合成了五种新的吡喹酮类似物:2-二硫代甲酸酯-1:2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a] 异喹啉-4-酮,动物实验筛选的结果表明化合物Vla、c、e治疗感染小鼠后的减虫率在10%左右,抗血吸虫作用较吡喹酮差.中间体2-苯甲酰基-1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉-4-酮的合成,采用相转移法,避免了原环合反应中的缺点.
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| 关 键 词： | 抗血吸虫病药 吡喹酮类似物 二硫代甲酸酯 |
SYNTHESIS OF 2-SUBSTITUTED-DITHIOFORMIC ACID ESTER ANALOGUES OF ANTISCHISTOSOMAL DRUG PRAZIQUANTEL |
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| Sckistosomiasis Reasearck Laboratory. SYNTHESIS OF 2-SUBSTITUTED-DITHIOFORMIC ACID ESTER ANALOGUES OF ANTISCHISTOSOMAL DRUG PRAZIQUANTEL[J]. Journal of Chongqing Medical University, 1988, 0(4) |
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| Authors: | Sckistosomiasis Reasearck Laboratory |
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| Affiliation: | Sckistosomiasis Reasearck Laboratory,Department of Chemistry Li Jiasheng and Chen Boyi |
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| Abstract: | In order to obtain antischistosomal agents by modification of the chemical structure of praziquantel, five compounds of 2-substituted dithioformic acid ester of 1, 2, 3, 6, 7, 11b-hexahydro-4H-pyrazine [2, 1-a] isoquinolinones Were synthesized.Screening with experimental, compound VIa, c and e showed lower activity against schistosomiasis japonicum in mice than praziquantel.2-Benzoyl-1, 2, 3, 6, 7, 11b-hexahydro-4H-pyrazine [2, 1-a] iscquinolin-4-ones, a key intermediate for the synthesis of praziquantel analogues, was prepared by utilizing phase transfer catalysis techniques in 86% yield from 1-benzoylaminomethyl- -chloroacetyl-1, 2, 3, 4-tetrahydro-isoquinolin |
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| Keywords: | Antischistosomal agents Praziquantel analogue Dithioformic acid ester |
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