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<p>The study of the kinetics of the reaction of sulfasalazine with picryl benzoate in aqueous 1,4-dioxane with a water content of 10 wt.% in a temperature range of 298–313 K revealed a low reactivity of sulfasalazine: the rate constants do not exceed <i>k</i>=(1.807±0.090) • 10<sup>−3</sup> L mol<sup>−1</sup> s<sup>−1</sup>. According to the results of virtual screening (using the PASS Online program) of the biological activity and toxicity of sulfasalazine and its <i>N</i>-benzoylated product, the reaction product has a reduced probability of insulin inhibition and antagonistic action against <i>p</i>-aminobenzoic acid, as well as nephro-, hepato- and hematotoxicity.</p>

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Benzoylation of sulfasalazine in aqueous 1,4-dioxane

  • 期刊论文

  • 发表日期：

    2025年3月1日

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  • T. P. Kustova,
  • K. A. Baturova,
  • M. S. Gruzdev,
  • L. B. Kochetova

摘要

The study of the kinetics of the reaction of sulfasalazine with picryl benzoate in aqueous 1,4-dioxane with a water content of 10 wt.% in a temperature range of 298–313 K revealed a low reactivity of sulfasalazine: the rate constants do not exceed k=(1.807±0.090) • 10−3 L mol−1 s−1. According to the results of virtual screening (using the PASS Online program) of the biological activity and toxicity of sulfasalazine and its N-benzoylated product, the reaction product has a reduced probability of insulin inhibition and antagonistic action against p-aminobenzoic acid, as well as nephro-, hepato- and hematotoxicity.