Abstract

“Double” derivatives of the drug Xymedon (1,2-dihydro-4,6-dimethyl-1-N-(hydroxyethyl)pyrimidone-2), hereafter referred to as pyrimidine (I), in which the pyrimidine (I) molecules are joined by an alkyl(xylylenyl)dionate bridge have been synthesized. Primary data on the hepatoprotective activity of five “double” pyrimidine (I) derivatives with different numbers of methylene groups and a meta-xylylene fragment in the ester bridge have been obtained on normal human hepatocytes of the Chang Liver cell line. The cytotoxicity and the cytoprotective properties of the new compounds against the background of exposure to d-galactosamine at a concentration of 150 mmol/L have been determined, their effect on the cell cycle compared with that of the initial pyrimidine (I) has been studied, and the dependence of the biological properties of the derivatives on their structure has been established.

中文翻译：

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“双重”嘧啶衍生物：体外保肝性能的合成和初步评估

摘要

药物Xymedon（1,2-二氢-4,6-二甲基-1-N-（羟乙基）嘧啶酮-2）的“双”衍生物，以下称为嘧啶（I），其中嘧啶（I）分子通过烷基（二甲苯基）二酸酯桥连接的三元共聚物已被合成。五个“双重”嘧啶（的保肝活性主数据予）具有不同数量的亚甲基基团和衍生物元在酯桥-xylylene片段已在常肝细胞系的正常的人肝细胞得到。新化合物在暴露于d的背景下的细胞毒性和细胞保护特性确定了浓度为150 mmol / L的β-半乳糖胺，研究了其与初始嘧啶（I）相比对细胞周期的影响，并确定了衍生物的生物学特性对其结构的依赖性。