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<p>To further explore and discover natural products-based antifungal agents, seventeen tertiary amide-oleanolic acid hybrids were designed and synthesized, and structurally confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR, HRMS, and melting point. Bioassay results illustrated that derivative <b>4&#xa0;k</b> exhibited prominent in vitro inhibitory activity against the mycelium growth of <i>Gaeumannomyces graminis</i> and <i>Valsa mali</i> with the EC<sub>50</sub> values of 41.77 and 43.96&#xa0;μg/mL, respectively. Meanwhile, the structure–activity relationships were also summarized. Moreover, in vivo control efficacy demonstrated that derivative <b>4&#xa0;k</b> displayed remarkable curative effect (CE) against<i> V. mali</i> at 200&#xa0;μg/mL with the value of 52.6%, evidently superior to that of the positive control carbendazim (41.5%). Besides, derivative <b>4&#xa0;k</b> also exhibited good CE against <i>Botrytis cinerea</i> at 200&#xa0;μg/mL with the value of 33.0%. Scanning electron microscope analysis initially indicated that derivative <b>4&#xa0;k</b> may exert its antifungal effect by leading to abnormal morphology on the mycelium surface, resulting in the aberrant hypha growth.</p> Graphical Abstract <p></p>

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Design and semisynthesis of novel oleanolic acid-based tertiary amide derivatives as promising antifungal agents against phytopathogenic fungi

  • 期刊论文

  • 发表日期：

    2025年2月11日

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  • Guoqing Sui,
  • Jiayi Sun,
  • Ailing Zhang,
  • Shuhua Cao,
  • Xiaobo Huang

摘要

To further explore and discover natural products-based antifungal agents, seventeen tertiary amide-oleanolic acid hybrids were designed and synthesized, and structurally confirmed by 1H NMR, 13C NMR, HRMS, and melting point. Bioassay results illustrated that derivative 4 k exhibited prominent in vitro inhibitory activity against the mycelium growth of Gaeumannomyces graminis and Valsa mali with the EC50 values of 41.77 and 43.96 μg/mL, respectively. Meanwhile, the structure–activity relationships were also summarized. Moreover, in vivo control efficacy demonstrated that derivative 4 k displayed remarkable curative effect (CE) against V. mali at 200 μg/mL with the value of 52.6%, evidently superior to that of the positive control carbendazim (41.5%). Besides, derivative 4 k also exhibited good CE against Botrytis cinerea at 200 μg/mL with the value of 33.0%. Scanning electron microscope analysis initially indicated that derivative 4 k may exert its antifungal effect by leading to abnormal morphology on the mycelium surface, resulting in the aberrant hypha growth.

Graphical Abstract