N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, 47 Leninsky Prosp., Moscow 119991, Russia.
Faculty of Chemical-Pharmaceutical Technologies and Biomedical Preparations, Mendeleev University of Chemical Technology, 9 Miusskaya Sq., Moscow 125047, Russia.
Int J Mol Sci. 2023 Mar 17;24(6):5756. doi: 10.3390/ijms24065756.
A series of S-alkyl substituted thioglycolurils was prepared through the alkylation of corresponding thioglycolurils with halogenoalkanes and tested for their fungicidal activity against six phytopathogenic fungi from different taxonomic classes: , , , , , and and two pathogenic yeasts: and . A number of S-alkyl substituted thioglycolurils exhibited high activity against and (85-100% mycelium growth inhibition), and moderate activity against other phytopathogens. S-Ethyl substituted thioglycolurils possessed a high activity against . Additionally, the hemolytic and cytotoxic properties of promising derivatives were determined using human red blood cells and human embryonic kidney cells, respectively. Two S-ethyl derivatives possessed both low cytotoxicity against normal human cells and high fungicidal activity against .
通过相应的硫代缩二脲与卤代烷的烷基化反应，制备了一系列 S-烷基取代的硫代缩二脲，并测试了它们对来自不同分类群的六种植物病原真菌和两种病原酵母的杀菌活性： ， ， ， ， ， 和 ， 。一些 S-烷基取代的硫代缩二脲对 和 （85-100%的菌丝生长抑制）表现出高活性，对其他植物病原菌表现出中等活性。S-乙基取代的硫代缩二脲对 具有高活性。此外，使用人红细胞和人胚肾细胞分别测定了有前途的衍生物的溶血和细胞毒性性质。两种 S-乙基衍生物对正常人类细胞的细胞毒性低，对 的杀菌活性高。
