抗血吸虫药物的研究Ⅴ——三(气六)化锑类型(R·HCl·SbCl_3)化合物,酒石酸锑钾衍生物与复合物等的制备

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[1] 由脂肪第三胺,芳香胺,杂环胺类在浓盐酸中与三氯化锑结合而成的R·HGI·SbCl_3类型的化合物(R=上述的胺类)均系结晶形的稳定化合物。本类型化合物对消灭日本血吸虫具有显著的作用。其中灭虫率在90%以上的有2-氨基毗啶锑,2-甲基吡啶锑,六氢毗啶锑,喹啉锑,三乙胺锑;灭虫率达100%的有尼可刹米锑,2-氨基嘧啶锑,N,N′-二甲基胡椒嗪锑等。此类化合物的灭虫作用,似主要决定于其组成中的SbCl_3,从与其相结合的胺类本身来看,似对疗效影响不大,但胺类本身毒性的大小,对生成物毒性的大小(除含锑量的高低对毒性有一定影响外),则具有较显著的影响。[2] 直接用三氯化锑,在一定的pH浓度下,于明胶水溶液中进行水介,再与鞣酸结合而成的一种缓介胶性锑化合物(鞣酸明胶锑),在小白鼠实验治疗中,经几次复筛,它的毒性比酒石酸锑钾要小得多,其灭虫率为94%。[3] 酒石酸锑钾与隣苯三酚结合成成水溶性复合物(酒石酸锑钾隣苯三酚)其毒性较酒石酸锑钾为低,而口服疗效比酒石酸锑钾为好。经几次复筛,其灭虫率为99.66—100%。又酒石酸2-氨基毗啶锑灭虫率亦达100%。[4] 过筛的几种非锑化合物,对日本血吸虫均无作用。本文全部化合物的元素分析由本院元素分析室何林兴、樊梅芳、薛绣鸿同志及分析教研组林力行同志进行。本文全部化合物的药理试验由药理教研组张颂,陈德标,陈品春同志进行。 [1] Compounds of the R · HGI · SbCl 3 type (R = the above-mentioned amines) composed of a fatty tertiary amine, an aromatic amine and a heterocyclic amine combined with antimony trichloride in concentrated hydrochloric acid all have a crystalline Stable compounds. This type of compound has a significant effect on the elimination of Schistosoma japonicum. Pest control rate of more than 90% of 2-amino pyridine side antimony, 2-methyl pyridine antimony, hexahydropyridine antimony, antimony quinoline, triethylamine antimony; pest control rate of 100% Antimony, 2-aminopyrimidine antimony, N, N’-dimethyl piperzine antimony and the like. The pest control effect of these compounds seems to be mainly determined by the composition of SbCl_3. The amines themselves combined with them seem to have little effect on the curative effect. However, the toxicity of amines themselves and the toxicity to the products (Except for the level of antimony has a certain impact on toxicity), then have a more significant impact. [2] directly with antimony trichloride, at a certain pH concentration in aqueous solution of gelatin in water, and then combined with tannic acid made of a gelatinized antimony compound (tannic acid gelatin antimony), small In the experimental treatment of rats, after several times of re-screening, its toxicity is much smaller than the antimony potassium tartrate, the pest control rate was 94%. [3] Antimony potassium tartrate combined with pyrogallol to form a water-soluble complex (antimony potassium tartrate pyrogallol) is less toxic than antimony potassium tartrate and orally more potent than antimony potassium tartrate. After several re-screening, the pest control rate of 99.66-100%. And 2-amino pyridine pyridine tartaric acid pest control rate of 100%. [4] Sifted several non-antimony compounds, Japan Schistosoma have no effect. The elemental analysis of all the compounds in this paper is carried out by Comrade Lin Liming, Fan Meifang, Xue Xiuhong and the Analytical Teaching and Research Section of the Element Analysis Office of the Institute. Pharmacological tests of all the compounds in this article were carried out by Zhang Song, Chen Debiao and Chen Pinchun of the Pharmacology and Research Group.
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