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Single-Step Enrichment of a TAP-Tagged Histone Deacetylase of the Filamentous Fungus Aspergillus nidulans for Enzymatic Activity Assay
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Novel 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Pyrimidin-4-ether Histone Deacetylase Inhibitors for Controlling
Xing-Hai Liu1, Chen-Hao Fu1,2, Jian Wang1,2
1College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
Journal of Agricultural and Food Chemistry
|February 12, 2025
Summary
New trifluoromethyloxadiazole (TFMO) fungicides show excellent rust control in crops. Compound XII6 effectively combats pathogens like *Puccinia pachyrhizi* and *Puccinia rubigo* with low toxicity, offering a promising alternative to existing treatments.
Area of Science:
- Agricultural Chemistry
- Plant Pathology
- Medicinal Chemistry
Background:
- Rust diseases caused by plant pathogens significantly reduce crop and fruit yields.
- Trifluoromethyloxadiazole (TFMO) compounds are known histone deacetylase inhibitors (HDACs).
Purpose of the Study:
- To design and synthesize novel TFMO-based pyrimidin-4-ether derivatives as potential fungicides.
- To evaluate the efficacy and safety of these compounds against key plant rust pathogens.
Main Methods:
- Synthesis of a series of 5-(trifluoromethyl)-1,2,4-oxadiazole (TFMO)-based pyrimidin-4-ether derivatives.
- Antirust bioassays against *Puccinia sorghi*, *Phakopsora pachyrhizi*, and *Puccinia rubigo*.
- Enzyme inhibition assays, acute toxicity tests, and structure-activity relationship (SAR) analysis.
Main Results:
- Several synthesized TFMO derivatives demonstrated excellent activity against plant rust pathogens.
- Compound XII6 showed superior control of *P. pachyrhizi* (50% at 0.780 mg/L) compared to azoxystrobin.
- Field trials confirmed compound XII6's efficacy against *P. rubigo* (116 g a.i./ha) with low acute toxicity.
- Compound XII6 was identified as a potent, nonselective HDAC inhibitor.
Conclusions:
- The study successfully developed novel TFMO-based pyrimidin-4-ether derivatives with significant fungicidal properties against rust diseases.
- Compound XII6 represents a highly effective and low-toxicity fungicide candidate for rust management in agriculture.
- Further optimization of compound XII6 is warranted for enhanced agricultural applications.
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