New 2-oxo-1,2-dihydropyrimidines: synthesis, cytotoxicity, and cytoprotective properties

IF 1.7 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY
M. S. Shashin, A. A. Parfenov, A. B. Vyshtakalyuk, G. P. Belyaev, M. M. Shulaeva, I. V. Galyametdinova, A. F. Saifina, A. T. Gubaidullin, V. V. Zobov, V. E. Semenov
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引用次数: 0

Abstract

New pyrimidine derivatives were synthesized in order to identify structural moieties of the anti-burn drug Xymedon (1-(2-hydroxyethyl)-4,6-dimethyl-2-oxopyrimidine) responsible for its hepatoprotective properties and to expand the range of hepatoprotectors based on the pyrimidine platform. For the newly synthesized compounds, the structure—cytotoxicity relationship and cytoprotective properties (against the toxic effect of d-galactosamine) were determined using human cell lines in comparison with Xymedon. The modification of structural moieties of Xymedon was shown to increase the cytotoxicity of isostructural pyrimidines; nevertheless, a significant cytoprotective effect was revealed for some of them. The structure of one new pyrimidine, 4,6-diethyl-1-(2-hydroxyethyl)-2-oxopyrimidine, was confirmed by X-ray diffraction.

新的2-氧-1,2-二氢嘧啶:合成、细胞毒性和细胞保护特性
为了鉴定抗烧伤药物Xymedon(1-(2-羟乙基)-4,6-二甲基-2-氧嘧啶)的肝保护特性的结构部分,并扩大基于嘧啶平台的肝保护范围,合成了新的嘧啶衍生物。对新合成的化合物进行了结构-细胞毒性关系和细胞保护性能(对d-半乳糖胺的毒性作用)的测定,并与Xymedon进行了比较。对Xymedon结构部分的修饰可提高同构嘧啶的细胞毒性;然而,其中一些具有明显的细胞保护作用。用x射线衍射证实了新嘧啶4,6-二乙基-1-(2-羟乙基)-2-氧嘧啶的结构。
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来源期刊
Russian Chemical Bulletin
Russian Chemical Bulletin 化学-化学综合
CiteScore
2.70
自引率
47.10%
发文量
257
审稿时长
3-8 weeks
期刊介绍: Publishing nearly 500 original articles a year, by leading Scientists from Russia and throughout the world, Russian Chemical Bulletin is a prominent international journal. The coverage of the journal spans practically all areas of fundamental chemical research and is presented in five sections: General and Inorganic Chemistry; Physical Chemistry; Organic Chemistry; Organometallic Chemistry; Chemistry of Natural Compounds and Bioorganic Chemistry.
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