Pest management science · 2025
Discovery of novel 1,5-diaryl-3-trifluoropyrazoles as antifungal pesticides for crop protection.
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Ma Yihui, Yang Dangwei, Qin Guangyu, Yang Jun, Sun Xianglong, Gao Xiaoyu
Аннотация
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 EC50 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 skeleton for antifungal pesticides development and provided compound 7 as a promising pesticide candidate for further development. © 2025 Society of Chemical Industry.
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 EC50 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 skeleton for antifungal pesticides development and provided compound 7 as a promising pesticide candidate for further development. © 2025 Society of Chemical Industry.