Discovery of novel 1,5‐diaryl‐3‐trifluoropyrazoles as antifungal pesticides for crop protection

作者：Yihui Ma, Dangwei Yang, Guangyu Qin, Jun Yang, Xianglong Sun, Xiaoyu Gao · 发表于：Pest Management Science · 年份：2025 · DOI：10.1002/ps.8909 · 被引用次数：3 · 研究领域：Fungal Plant Pathogen Control、Plant Disease Resistance and Genetics、Plant Pathogens and Fungal Diseases

Abstract BACKGROUND Plant diseases caused by phytopathogenic fungi continue to threaten global food security, driving the urgent need for discovery of antifungal agrochemicals with novel modes of action. The motif of 1,5‐diaryl‐3‐trifluoropyrazole was found to be associated with potential antifungal effect and HNNK‐5 was such an agrochemical being developed in our lab with moderate potency. This study took HNNK‐5 as the parent compound for lead optimization to discovery novel fungicides. RESULT To further explore the antifungal potential of this class of compounds, a series of analogues of HNNK‐5 was designed and prepared. Among them, compound 7 was identified as the most potent member with much improved activity over the lead compound. Compound 7 almost completely inhibited the growth of all the tested fungal pathogens at 50 μg/mL with an EC 50 range of 6.2–11.5 μg/mL, multiple‐fold less potent than the positive control azoxystrobin. Scanning electronic microscope (SEM) observation and fatty acid analysis showed that compound 7 treatment caused morphological changes and altered the amount of fatty acids of Fusarium oxysporum . Furthermore, compound 7 at higher application rates showed pronounced controlling effects against peanut root rot disease caused by Fusarium oxysporum in field study, similar to those of positive control azoxystrobin. CONCLUSION This study indicated that the characteristic structure of 1,5‐diaryl‐3‐trifluoropyrazole could be employed as a potential ske...