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<p>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 <i>d</i>-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.</p>

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

  • 期刊论文

  • 发表日期：

    2025年4月1日

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  • 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

摘要

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.