(新抗真菌的。7n -芳基二硫代氨基甲酸酯和氨基氯化物(作者译)]。

T Zsolnai
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引用次数: 0

摘要

生成了若干n -芳基二硫代氨基甲酸酯及其n -甲基衍生物,并比较了这些化合物的抑菌作用。结果表明,n -芳基二硫代氨基甲酸酯具有广泛的抑菌活性,但其n -甲基衍生物在这方面完全无活性。n -芳基二硫代氨基甲酸酯很容易转化为芳基异硫氰酸酯,但它们的n -甲基衍生物不能实现这种转化。这些事实间接证明n -芳基二硫代氨基甲酸酯确实通过原位形成芳基异硫氰酸酯发挥抑菌作用。研究了几种芳基和芳烷基氨基氯化物的抑菌作用。同时考察了相应的芳基异硫氰酸酯和芳烷基异硫氰酸酯的抑菌效果,以确定这两种相似类型的化合物在抑菌效果强度上是否存在差异。结果表明,所检测的芳基和芳烷基基氨基氯化物具有较强的抑菌作用,但其抑菌活性低于相应的芳基和芳烷基异硫氰酸酯。结果表明,芳基异硫氰酸酯的抑菌活性因其分子间位或对位上的氯原子或对位上的溴原子而明显增加,而芳基氨基氯化物的抑菌活性因其分子间位或对位上的氯原子而明显降低,相反,这两类化合物的抑菌活性均因3,4-二氯取代而增加。
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[Newer antimycotics. VII. N-aryl-dithiocarbamic-esters and carbylaminochlorides (author's transl)].

A number of N-aryl-dithiocarbamic-esters and their N-methyl-derivatives are produced and the fungistatic action of these compounds compared with one another. It was demonstrated that N-aryl-dithiocarbamic-esters exert an intensive fungistatic action with a wide spectrum of activity, but their N-methyl-derivatives are in this respect totally inactive. The N-aryl-dithiocarbamic-esters are transformed easily into arylisothiocyanates, but their N-methyl-derivatives are unable to effect such transformation. These facts provide an indirect evidence of N-aryl-dithiocarbamic-esters to exert their fungistatic effect indeed by the formation of arylisothiocyanates in situ. The fungistatic action of a number of aryl- and aralkyl-carbylaminchlorides, respectively, was examined. The fungistatic effect of the corresponding aryl- and aralkyl-isothiocyanates was examined in parallel to decide whether a difference between these two similar types of compounds in the intensity of their fungistatic effect exists. It was demonstrated that the examined aryl- and aralkyl-carbylaminchlorides exert an intensive fungistatic effect, but their fungistatic activity is less intensive than that of the corresponding aryl- and aralkyl-isothiocyanates. It was furthermore demonstrated that the fungistatic activity of aryl-isothiocyanates is considerably increased by a chlorine atom in the meta or para position or by a bromine atom in the para position of their molecules, but the fungistatic action of the aryl-carbylaminchlorides is significantly decreased by this on the contrary, the fungistatic activity of both series of compounds is increased by 3,4-dichloro substitution.

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