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<p>Novel derivatives of A-secooleanolic and A-secobetulinic acids containing a propargylamine substituent at the C(28) position were synthesized <i>via</i> the Cu-catalyzed Mannich reaction. Antiviral properties of the compounds were evaluated on MDCK cell culture against influenza A/Puerto Rico/8/34 (H1N1) virus. It was demonstrated that among the Mannich bases of A-secooleanolic acid, the derivative containing the piperazine moiety exhibited the highest activity (IC<sub>50</sub> = 5 µmol L<sup>−1</sup> and SI &gt;100). In the case of A-secobetulinic acid, a positive effect was caused by the introduction of <i>N</i>-methylpiperazine (IC<sub>50</sub> = 1 µmol L<sup>−1</sup> and SI &gt;25) and morpholine (IC<sub>50</sub> = 3 µmol L<sup>−1</sup> and SI = 42) moieties.</p>

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Antiviral activity of Mannich bases linked to A-secotriterpenoids at the C(28) position

  • 期刊论文

  • 发表日期：

    2025年3月1日

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  • A. V. Petrova,
  • Ya. L. Esaulkova,
  • M. G. Mikhalsky,
  • V. V. Zarubaev,
  • O. B. Kazakova

摘要

Novel derivatives of A-secooleanolic and A-secobetulinic acids containing a propargylamine substituent at the C(28) position were synthesized via the Cu-catalyzed Mannich reaction. Antiviral properties of the compounds were evaluated on MDCK cell culture against influenza A/Puerto Rico/8/34 (H1N1) virus. It was demonstrated that among the Mannich bases of A-secooleanolic acid, the derivative containing the piperazine moiety exhibited the highest activity (IC50 = 5 µmol L−1 and SI >100). In the case of A-secobetulinic acid, a positive effect was caused by the introduction of N-methylpiperazine (IC50 = 1 µmol L−1 and SI >25) and morpholine (IC50 = 3 µmol L−1 and SI = 42) moieties.