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[具有抗真菌活性的双-(2-羧基苯基)-二硫化物的伯酰胺]

[Primary amides of bis-(2-carboxyphenyl)-disulfides with antimycotic activity].

作者信息

Montanari L, Mazza M, Pavanetto F

出版信息

Farmaco Sci. 1977 Jul;32(7):539-48.

PMID:330218
Abstract

A series of bis-amides of 2,2'-dicarboxydiphenyldisulfides with monosubstituted N-alkyl groups (substances I leads to XXVI) or N-aralkyl groups (substances XXVI leads to XLII) was prepared and examined for in vitro antifungal activity. The substances were obtained by condensing the chloride of 2,2'-dicarboxydiphenyldisulfide with suitable amines. The fungistatic activity of the products was tested in vitro against the following four strains: Candida albicans, Candida tropicalis, Saccharomyces cerevisiae, Trichophyton mentagrophytes. The results obtained summarised in Tables I and II amplify the structure-antifungal activity relationships of this class of compound. The most active compounds proved to be bis-(N-n.heptyl-2-carboxami-dophenyl)disulfide (XX) and bis-(N-beta-4Cl-phenylethyl-2-carboxamidophenyl)disulfide (XXXV).

摘要

制备了一系列2,2'-二羧基二苯基二硫化物与单取代N-烷基(物质I至XXVI)或N-芳烷基(物质XXVI至XLII)的双酰胺,并对其体外抗真菌活性进行了研究。这些物质是通过使2,2'-二羧基二苯基二硫化物的氯化物与合适的胺缩合而得到的。在体外针对以下四种菌株测试了产物的抑菌活性:白色念珠菌、热带念珠菌、酿酒酵母、须癣毛癣菌。表I和表II中总结的结果进一步说明了这类化合物的结构与抗真菌活性之间的关系。最具活性的化合物被证明是双-(N-正庚基-2-羧酰胺基苯基)二硫化物(XX)和双-(N-β-4-氯苯乙基-2-羧酰胺基苯基)二硫化物(XXXV)。

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