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<p>Plant-parasitic nematode (PPNs) infections threaten global crop protection and result in substantial annual losses to agriculture worldwide. However, only a limited number of nematicides are currently available, and drug resistance is becoming a more significant concern. Therefore, there is an urgent need to develop new, highly effective, and environmentally friendly nematicides. This study designed and synthesized forty-two novel fluopyram analogues containing five-membered heterocyclic molecules <i>via</i> a “Ring Replacement” strategy. Results from the nematicidal activity testing showed that all the target compounds showed certain activity against <i>Caenorhabditis elegans</i>. Notably, compound <b>21r</b> demonstrated an LC<sub>50</sub> value of 1.83&#xa0;mg/L, which is significantly lower than that of the commercial nematicide, tioxazafen, but slightly higher than that of the SDHI nematicide, fluopyram. Enzymatic assays and molecular docking studies identified nematode SDH as the probable molecular target. An ecological and environmental risk assessment was also conducted on the target compound <b>21r</b>. However, the long-term toxic effects of these compounds on aquatic life remain to be further explored. The study indicates that the thiophene moiety, a five-membered heterocyclic ring system, holds significant potential for developing novel SDHI nematicides. The results provide critical mechanistic insights and lay the groundwork for the development of novel nematicides, which will contribute to improving crop protection strategies in agriculture.</p>

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Fluopyram analogues containing a five-membered heterocyclic ring moiety: synthesis, nematicidal activity and molecular docking study

  • 期刊论文

  • 发表日期：

    2026年2月19日

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  • Zhitian Huang,
  • Shenghong Jing,
  • Qianyu Huang,
  • Jie Chu,
  • Hao Ling,
  • Jiayi Wang,
  • Gonghua Song

摘要

Plant-parasitic nematode (PPNs) infections threaten global crop protection and result in substantial annual losses to agriculture worldwide. However, only a limited number of nematicides are currently available, and drug resistance is becoming a more significant concern. Therefore, there is an urgent need to develop new, highly effective, and environmentally friendly nematicides. This study designed and synthesized forty-two novel fluopyram analogues containing five-membered heterocyclic molecules via a “Ring Replacement” strategy. Results from the nematicidal activity testing showed that all the target compounds showed certain activity against Caenorhabditis elegans. Notably, compound 21r demonstrated an LC50 value of 1.83 mg/L, which is significantly lower than that of the commercial nematicide, tioxazafen, but slightly higher than that of the SDHI nematicide, fluopyram. Enzymatic assays and molecular docking studies identified nematode SDH as the probable molecular target. An ecological and environmental risk assessment was also conducted on the target compound 21r. However, the long-term toxic effects of these compounds on aquatic life remain to be further explored. The study indicates that the thiophene moiety, a five-membered heterocyclic ring system, holds significant potential for developing novel SDHI nematicides. The results provide critical mechanistic insights and lay the groundwork for the development of novel nematicides, which will contribute to improving crop protection strategies in agriculture.