防治血吸虫病药物的研究Ⅳ.几个口服锑剂的合成

Wiley在1951年合成了一类毒性较低和口服有效的锑剂硫代水杨酸氯化锑化合物(Ⅰ),我们曾重复制备I_a及I_b,提供动物试验.文献曾报导氨基化合物的锑络合物对动物感染日本血吸虫病有口服疗效.综合文献的结果,我们考虑含有巯基的杂环化合物可能与锑形成较稳定的化合物,这样也许会减轻毒性及副作用,同时口服后可能易于掌握其肠胃道吸收规律,因此,我们用三氯化锑与2-甲基-1,3-二氮茚及2-巯基-1,3-硫氮茚分别在苯中加热,生成相应的含锑化合物Ⅱ及Ⅲ.其结构尚未能肯定.

STUDIES ON ANTIBILHARZIAL DRUGS——Ⅳ.SYNTHESES OF SOME ANTIMONIAL COMPOUNDS

Four antimonial compounds were prepared. Dichloro-(α-carbomethoxyphenyl) -thio- antimonite and dichloro- (α-carbethoxyphenyl)thioantimoni were prepared by the action of antimony trichloride on methyl and ethyl esters of thiosalicylic acid respectively. 2-Methyl-1,3-benzimidazole and 2-mercapto-benzothiazole were heated with antimony trichloride in benzene. Two corresponding antimonial compounds were obtained. The structure of these tWo compounds have not been determined as yet. These four compounds were tested for therapeutic effect on schistosomiasis japonica in mice and was compared with tartar emetic. It was found that they had higher effec- tiveness than tartar emetic when higher dosages (by weight) were used.