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血吸虫病化学治疗的研究——ⅩⅩⅤ.取代香豆素-3-羧酸酯和酰胺衍生物的合成
CHEMOTHERAPEUTIC STUDIES ON SCHISTOSOMIASIS ⅩⅩⅤ DERIVATIVES OF SUBSTITUTED COUMARIN-3-CARBOXYLIC ESTERS AND AMIDES
【摘要】 香豆素含有内酯结构时,可能有驱蠕效力。因此合成了取代香豆素-3-羧酸酯与酰胺化合物57个,经动物筛选发现6个化合物在感染日本血吸虫的小白鼠体内有显著驱蠕虫作用,其中以6-溴-香豆素-3-羧酸乙酯杀虫效力最强,试用于临床,证明有一定疗效。
【Abstract】 Some coumarin compounds containing a lactone ring have definite anthelmintic effect. Thus, fifty seven compounds of substituted coumarin-3-carboxylic esters and amides have been synthesized.After screening with mice, six of them were found to possess pronounced anthelmintic activity against Schistosomiasis japonica, among which ethyl 6-bromo-coumarin-3-carboxylate was shown to be the most effective and has passed on to clinical trials with promising results.
- 【文献出处】 药学学报 ,Acta Pharmaceutica Sinica , 编辑部邮箱 ,1982年01期
- 【被引频次】10
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