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1.从临床上口服有效的SbO-酯中分离出了氧氯化锑混合物苯巯基乙酸乙酯以及它的水介产物苯巯基乙酸等,确证了对-羧-甲巯基苯(月弟)酸在盐酸-酒精溶液中,有碘化钾存在下,用二氧化硫进行较长时间的还原过程中,使锑与苯环上碳原子结合的链断裂,无机锑即溶介在盐酸-酒精溶液中形成了三氯化锑,同时产生了由对-羧甲巯基苯(月弟)酸乙酯分介而来的苯巯基乙酸乙酯的油状物。2.经化学与药理试验,原SbO-酯主要由氧氯化锑混合物与苯巯基乙酸乙酯所组成,经分离出的氧氯化锑混合物的结晶与经分馏而获得的苯巯基乙酸乙酯分别进行药理试验的结果。前者对血吸虫有很高的作用,后者则无效。3.用新鲜制得的对-羧-甲巯基苯(月弟)酸,在酒精-盐酸溶液中用二氧化硫还原而得二氯-对-羧甲巯基苯(月弟)乙酯(原拟合成的芳香族锑化物的中同体),并制成了它的对硝基苯巯基化合物的衍生物等,经药理试验,疗效均不显著。4.用不同批号的S.J.59进行了将近200只小白鼠的口服实验治疗,(其毒性较吐酒石约低一倍,用等毒量进行治疗时,其灭虫率显较吐酒石口服为高),灭虫率达95-98%,并进行了四只家犬的实验治疗观察(其中两犬系由无锡血吸虫研究所协作进行),其中两犬的灭虫率达100%,其余两犬,一为83.5%,一为54.3%。S.J.66亦进行了不同批号的小白鼠实验治疗,其毒性与吐酒石相仿,灭虫率为89.3-95%。并进行了两只家犬的实验治疗,其灭虫率:一犬为79.9%,一犬为59.4%, 本文各化合物之分析结果由我院分析教研组林力行同志及元素分析室何林兴、凡梅芳等同志完成。
1. Isolation of ethyl mercaptoacetate and its mercaptoacetic acid as a mixture of antimony oxychloride and clinically orally available SbO-esters confirmed that p-carboxy-methylmercaptobenzene In hydrochloric acid - alcohol solution, in the presence of potassium iodide, with sulfur dioxide for a long time reduction process, so that antimony and benzene ring carbon atoms of the chain fracture, inorganic antimony namely hydrochloric acid - alcohol solution formed trichloride Antimony, at the same time produced by the p-carboxymethyl mercaptobenzene (Yue brother) ethyl ester of ethyl ester of ethyl mercaptoacetate from the oil. 2. By chemical and pharmacological tests, the original SbO-ester is mainly composed of antimony oxychloride mixture and ethyl mercaptoacetate composition, the crystallization of the mixture of antimony oxychloride and obtained by fractionation ethyl benzene mercaptoacetate Respectively pharmacological test results. The former has a high role for schistosomes, while the latter is ineffective. 3. With freshly prepared p-carboxymethylthiobenzene (cousin) acid in alcohol - hydrochloric acid solution was reduced with sulfur dioxide to give dichloro-p-carboxymethyl mercaptophenyl benzene (cousin) ethyl ester (the original fit Into the aromatic stilbite), and made it on the nitrobenzene mercapto compounds such as derivatives, the pharmacological tests, the curative effect is not significant. 4. With different batches of SJ59 conducted nearly 200 mice oral experimental treatment, (its toxicity about twice as spit tortoise, with the same dose of treatment, the pest control rate was significantly higher than spit tartar As high), pest control rate of 95-98%, and the experimental treatment of four dogs were observed (of which two dogs by the Institute of Schistosoma Schistosoma infection cooperation), of which the two dogs off the rate of 100%, the rest Two dogs, one was 83.5%, one was 54.3%. S.J.66 also conducted different batches of mice experimental treatment, its toxicity and spit tartar, pest control rate of 89.3-95%. And the experimental treatment of two domestic dogs, the rate of pest control: a dog was 79.9%, a dog was 59.4%, the analysis results of the compounds in this article by our hospital analysis and research group Comrade Lin Lihang and elemental analysis of the Office of He Linxing, Fan Mei Fang and other comrades completed.