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化学学报
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化学学报 ›› 1957, Vol. 23 ›› Issue (2): 105-111. 上一篇    下一篇

论文

血吸蟲病化學治療的研究Ⅱ.幾種巯基羧酸的銻衍生物

謝毓元, 章辛, 楊行忠, 嵇汝運   

  1. 中国科学院药物研究所
  • 投稿日期:1956-11-14 发布日期:2013-06-03

CHEMOTHERAPEUTIC STUDIES ON SCHISTOSOMIASIS Ⅱ. ANTIMONY DERIVATIVES OF SOME MERCAPTOCARBOXYLIC ACIDS

HSIEH YU-YUAN, CHANG SING, YANG IN-TSON, KYI ZU-YOONG   

  1. Institute of Materia Medica, Academia Sinica, Shanghai
  • Received:1956-11-14 Published:2013-06-03

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2,3-二疏基丙酸与三氯化锑缩合时形成2-氯-4-羧基-4,5-二氢-1,3-二间硫锑杂茂(Ⅵ:R=H),这个产物的氯原子在水解为羟基时,随同失去一分子水而成为内鹽(Ⅶ)。 2,3-二巯基丁二酸能与酒石酸锑钾起复分解作用,生成环状硫醇盐[4,5-二羧基-4,5-二氢-2-羟基-1,3-二间疏锑杂茂(V)]:但当2,3-二巯基丁二酸与三氯化锑作用,并用碳酸氢钠除去氯化氢时,生成与Friedheim所述“TWSb”(X)成分相同的物质。将内消旋2,5-二巯基已-1,6-二酸与酒石酸锑钾处理时得到4,7-二羧基-1,3-二间硫-2-羟锑杂环庚烷单钾盐(Ⅺ)。这些产物曾用於小白鼠的日本血吸虫病实验治疗,其中Ⅶ及Ⅺ的疗效较酒石酸锑钾为好。

Attempts have been made to prepare less toxic antimonials for use in chemotherapy on Schistosomiasis japonicum.It has been established[5] that 2,3-dimercaptopropanol is a powerful antilewisite because it forms a stable ring compound (Ⅱ) with arsenic.It seems reasonable to suppose that analogous cyclic antimony mercaptides (such as IV and V) should ibe difficult to dissociate and therefore would be less toxic.