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Background <p>Root-knot nematodes, particularly <i>Meloidogyne incognita</i>, cause severe yield losses in a wide range of crops, necessitating the development of new chemical scaffolds to overcome limitations associated with conventional nematicides. High mortality observed during the initial screening of the Korea Chemical Bank library identified compound <b>64302,</b> as a promising hit. However, its furan core presented intrinsic stability issues, prompting a thiophene-based redesign aimed at developing stable and effective nematicidal agents.</p> Results <p>Structural optimization of the hit compound led to the synthesis of a series of thiophene-guanidinylamide derivatives. Among the 32 synthesized candidates, compounds <b>6a</b>, <b>6d</b>, and <b>6e</b> exhibited 100% in vitro mortality against second-stage juveniles of <i>Meloidogyne incognita</i> at 1.0&#xa0;mg L⁻¹. Structure-activity relationship analysis revealed that a 2-nitro substituent on the A-ring was essential for activity, while the guanidinylamide moiety and thiophene B-ring were also critical structural features. In greenhouse assays, the three lead compounds showed dose-dependent suppression of root galling, with <b>6e</b> demonstrating complete control across all tested concentrations (50–450 mg L<sup>− 1</sup>). Unlike cadusafos, compound <b>6e</b> showed no phytotoxicity, indicating a favorable safety margin together with strong nematicidal performance.</p> Conclusion <p>This study identifies thiophene-guanidinylamides as a new class of potent nematicidal agents with high in vitro and in vivo efficacy against <i>Meloidogyne incognita</i>. The superior performance and lack of phytotoxicity observed for compound <b>6e</b> highlight its potential as a promising lead scaffold for the development of next-generation nematicides.</p> Graphical Abstract <p></p>

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Design, synthesis, and evaluation of thiophene-guanidinylamides as potent nematicidal agents against Meloidogyne incognita

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年5月3日

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  • Ji Hye Choi,
  • Seo Yeon Kim,
  • Yong Ho Choi,
  • Gyung Ja Choi,
  • Hee Nam Lim,
  • Hyun-Suk Yeom

摘要

Background

Root-knot nematodes, particularly Meloidogyne incognita, cause severe yield losses in a wide range of crops, necessitating the development of new chemical scaffolds to overcome limitations associated with conventional nematicides. High mortality observed during the initial screening of the Korea Chemical Bank library identified compound 64302, as a promising hit. However, its furan core presented intrinsic stability issues, prompting a thiophene-based redesign aimed at developing stable and effective nematicidal agents.

Results

Structural optimization of the hit compound led to the synthesis of a series of thiophene-guanidinylamide derivatives. Among the 32 synthesized candidates, compounds 6a, 6d, and 6e exhibited 100% in vitro mortality against second-stage juveniles of Meloidogyne incognita at 1.0 mg L⁻¹. Structure-activity relationship analysis revealed that a 2-nitro substituent on the A-ring was essential for activity, while the guanidinylamide moiety and thiophene B-ring were also critical structural features. In greenhouse assays, the three lead compounds showed dose-dependent suppression of root galling, with 6e demonstrating complete control across all tested concentrations (50–450 mg L− 1). Unlike cadusafos, compound 6e showed no phytotoxicity, indicating a favorable safety margin together with strong nematicidal performance.

Conclusion

This study identifies thiophene-guanidinylamides as a new class of potent nematicidal agents with high in vitro and in vivo efficacy against Meloidogyne incognita. The superior performance and lack of phytotoxicity observed for compound 6e highlight its potential as a promising lead scaffold for the development of next-generation nematicides.

Graphical Abstract