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Abstract <p> A molecular hybridization strategy was employed to synthesize 12 pyrazole hydrazide derivatives incorporating a thiazole fragment as potential antifungal agents. The newly synthesized compounds were systematically characterized using various techniques, including <sup>1</sup>H and <sup>13</sup>C NMR, ESI-MS, and elemental analysis. Notably, compound <b>4f</b> exhibited a high inhibition rate against <i>Valsa mali</i>, particularly in in vivo experiments, where it demonstrated significantly superior antifungal activity compared to the commercially available fungicide fluxapyroxad. Furthermore, molecular docking analysis provided a rational explanation for the differences in antifungal efficacy between compound <b>4f</b> and fluxapyroxad.</p>

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Design, Synthesis, and Antifungal Evaluation of Thiazole-Containing Pyrazole Hydrazide Derivatives

  • 期刊论文

  • 发表日期：

    2025年10月1日

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  • J. Yan,
  • Z. Yan,
  • Q. Han,
  • R. Huang,
  • X. Kang,
  • F. Gu

摘要

Abstract

A molecular hybridization strategy was employed to synthesize 12 pyrazole hydrazide derivatives incorporating a thiazole fragment as potential antifungal agents. The newly synthesized compounds were systematically characterized using various techniques, including 1H and 13C NMR, ESI-MS, and elemental analysis. Notably, compound 4f exhibited a high inhibition rate against Valsa mali, particularly in in vivo experiments, where it demonstrated significantly superior antifungal activity compared to the commercially available fungicide fluxapyroxad. Furthermore, molecular docking analysis provided a rational explanation for the differences in antifungal efficacy between compound 4f and fluxapyroxad.