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<p>In order to find more compounds with antifungal activities, a series of new compounds were designed and synthesized using the natural product of diterpenoid lactones, andrographolide, as the parent nucleus. Target compounds were identified by <sup>1</sup>H NMR, <sup>13</sup>C NMR and/or HR-MS. The bioassay results demonstrated that compound <b>4d</b> exhibited inhibition rates of over 60% against six fungal strains at 100&#xa0;<i>µ</i>g/mL, and the EC<sub>50</sub> value of <b>4d</b> against <i>P. piricola</i> was only 9.09 <i>µ</i>g/mL. SEM test showed that <b>4d</b> could damage the mycelia of <i>P. piricola.</i> obviously. Moreover, <b>4d</b> had no effect on cowpea seed germination, showing high safety.</p>

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Design, synthesis, and antifungal activity of 14-aryloxy/amide substituted andrographolide derivatives

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2025年11月25日

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  • Zhuyun Liu,
  • Shanshan Yang,
  • Jierui Ma,
  • Yunying Sha,
  • Yuyan Zhou,
  • Zhuqing Liu,
  • Lizhong Wang

摘要

In order to find more compounds with antifungal activities, a series of new compounds were designed and synthesized using the natural product of diterpenoid lactones, andrographolide, as the parent nucleus. Target compounds were identified by 1H NMR, 13C NMR and/or HR-MS. The bioassay results demonstrated that compound 4d exhibited inhibition rates of over 60% against six fungal strains at 100 µg/mL, and the EC50 value of 4d against P. piricola was only 9.09 µg/mL. SEM test showed that 4d could damage the mycelia of P. piricola. obviously. Moreover, 4d had no effect on cowpea seed germination, showing high safety.