关于血吸虫病药物的研究 Ⅰ.硫代水楊酸类化合物的合成
STUDIES ON ANTIBILHARZIAL DRUGS Ⅰ. SYNTHESES OF THIOSALICYLIC ACID DERIVATIVES
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摘要: 利用硫代水杨酸和它的甲基、丁基、苄基醚、以及双硫代水杨酸为原料,与β-二乙氨基氯乙烷及β-(1-六氢吡啶基)-氯乙烷在异丙醇中起Horenstein与Pahlicke反应,制成六个碱性酯类化合物的盐酸盐.曾由中国科学院药物研究所对这六个化合物进行治疗日本血吸虫病动物疗效试验,初步认为对小白鼠无治疗效果.Abstract: Methyl, butyl, and benzyl ethers of thiosalicylic acid or dithiosalicylic acid were used as starting materials to undergo Horenstein and Pahlicke esterification reaction with β-diethylaminoethyl chloride and β-piperidinoethyl chloride in isopropyl alcohol respectively. Six basic ester hydrochlorides were thus prepared. These compounds were tested for therapeutic effect on schistosomiasis japonica in mice. No curative effect was observed.
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