AI Article Synopsis

  • Downy mildew is a significant fungal threat to crops, with increasing resistance to current fungicides, highlighting the need for new treatments.
  • Researchers developed and tested a series of pyrazole amide derivatives for their effectiveness against the fungus Pseudoperonospora cubensis, responsible for cucumber downy mildew.
  • Among the compounds, T24 showed the best fungicidal activity and was further analyzed to understand how its structure contributes to its effectiveness, suggesting it could be a promising new fungicide.

Article Abstract

Background: Downy mildew is one of the major fungi causing significant economic losses to crops. The resistance of this fungus to current fungicides is increasing and new fungicides with a unique mode of action are needed.

Objective: To find a novel pyrazole amide derivative as a potential fungicide.

Methods: A series of pyrazole-5-carboxamide derivatives containing a diaryl ether were designed and synthesized by the Intermediate derivatization method (IDM). Their fungicidal activities against Pseudoperonospora cubensis (P. cubensis, cucumber downy mildew) were evaluated in the greenhouse.

Results: Bioassays indicated that several compounds exhibited excellent fungicidal activity against P. cubensis in vivo. In particular, T24 (EC = 0.88 mg L) had the highest activity compared with Dimethomorph and Fluazinam and other analogues. The relationship between the activity and the structure of these derivatives was analyzed, and an accurate and reliable three-dimensional quantitative structure-activity relationship (3D-QSAR) model was established to determine that electrostatic and steric fields had important effects on the improvement of fungicidal activity.

Conclusion: The novel pyrazole-5-carboxamide derivative T24 can be considered a potential fungicide for P. cubensis control.

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Source
http://dx.doi.org/10.2174/1570179420666230327145745DOI Listing

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