Zsolnai T
Zentralbl Bakteriol Orig A. 1976 Jan;234(1):110-20.
The author produced a number of aryl-hydrazone-derivatives of the esters and amides of mesoxalic-acid-seminitril and of mesoxalic-acid-diethylester, investigated their fungistatic efficiency in vitro, and discussed the association of chemical structure with the fungistatic effect in the series of these compounds. From the author's results it can be concluded that some compounds from the series of the aryl-hydrazones of mesoxalic-acid-seminitril-esters exert a strong fungistatic effect on Trichophyton gyps. (Tabl. 1); namely those, whose ester-alkyl-group is relatively short and in that there are the substituents of benzolring Cl-atom, CH3- or NO2- groups. On the other hand the majority of the compounds of this series is totally ineffective (Tab. 2). Each aryl-hydrazones of the amides of mesoxalic-acid-seminitril ant that ones of the mesoxalic-acid-diethylester are ineffective on Trichophyton gyps. (Tab. 2, 4, 5). Not a compound of the investigated series exerts any fungistatic effect on fungi-strains other then Trichophyton gyps. Those aryl-hydrazones of the mesoxalic-acid-seminitrilesters, which proved to be most effective on Trichophyton gyps. are on the mouse only negligible toxic and they do not irritate the skin and mucous membranes of the experimental animals; their fungistatic effect is not influenced by cystein, cysteamin or thioglycolic-acid. On the basis of the intensive fungistatic efficiency and small toxicity of some aryl-hydrazones of the mesoxalic-acid-seminitril-esters, it seems that a number of representatives of these types of chemical compounds could be given a role in the chemotherapy of superficial human and animal dermatomycoses.
作者制备了中草酸半腈酯和中草酸二乙酯的酯类及酰胺类的多种芳基腙衍生物，研究了它们的体外抑菌效率，并探讨了这些化合物系列中化学结构与抑菌效果之间的关联。从作者的结果可以得出结论，中草酸半腈酯的芳基腙系列中的某些化合物对石膏样毛癣菌具有很强的抑菌作用（表1）；也就是说，那些酯烷基相对较短且苯环上有氯原子、甲基或硝基取代基的化合物。另一方面，该系列的大多数化合物完全无效（表2）。中草酸半腈酰胺的每种芳基腙以及中草酸二乙酯的那些芳基腙对石膏样毛癣菌均无效（表2、4、5）。所研究系列中的任何一种化合物对除石膏样毛癣菌之外的真菌菌株均无抑菌作用。那些被证明对石膏样毛癣菌最有效的中草酸半腈酯的芳基腙对小鼠的毒性仅可忽略不计，且它们不会刺激实验动物的皮肤和黏膜；它们的抑菌作用不受半胱氨酸、半胱胺或巯基乙酸的影响。基于中草酸半腈酯的某些芳基腙的强效抑菌效率和低毒性，似乎这些类型的化合物中的许多代表物可在人类和动物浅表皮肤真菌病的化疗中发挥作用。
