Author

Dandan Wang

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Sep 2026

Discovery of Thiram-Inspired Thiocarbamate Derivatives as Novel Laccase Inhibitors against Sclerotium rolfsii

Peanut stem rot, caused by the soil-borne pathogen Sclerotium rolfsii, poses a significant threat to global peanut production and results in substantial yield losses. A series of thiocarbamate derivatives were synthesized and evaluated against ten phytopathogenic fungi. Over 50% showed broad-spectrum fungicidal activity at 40 mg/L. Notably, compound b6 exhibited superior activity against S. rolfsii (EC50 = 0.75 mg/L), surpassing Thiram (EC50 = 0.91 mg/L). In vivo assays confirmed robust protective and curative efficacies on peanut seedlings. b6 also demonstrated potent laccase inhibition (IC50 = 0.064 mmol/L), significantly outperforming l-cysteine (IC50 = 0.551 mmol/L) and PMDD-5Y (IC50 = 0.326 mmol/L). Mechanistic studies revealed that b6 disrupts fungal cell membrane integrity and induces intracellular ROS accumulation. Overall, b6 represents a promising antifungal lead compound for designing novel laccase inhibitor-based fungicides.

Rong Li, Yuan-Jian Huang, Min Ge et al. · Journal of Agricultural and... · 0 citations

Jul 2026

Molecular Concatenation of 3,5-Dichloro-2,6-Difluoropyridin-4-amine with Heterocyclic Carboxylic Acids and Evaluation of their Antifungal Activity.

Succinate dehydrogenase (SDH) inhibitors face cross-resistance issues due to similar structures. To address this problem, we designed heterocyclic carboxamide derivatives based on a 3,5-dichloro-2,6-difluoropyridin-4-amine scaffold. Compounds A1 and A2 showed excellent antifungal activity against Rhizoctonia solani (EC50 = 1.08 and 1.18 mg/L), outperforming boscalid (EC50 = 1.82 mg/L). They also exhibited broad-spectrum activity against four pathogenic fungi. In vivo rice leaf tests confirmed good protective effects (A1 and A2 at 92.88% and 89.35%, respectively). Mechanistic studies revealed that A1 and A2 disrupt mycelial morphology (Scanning electron microscopy analysis and transmission electron microscopy analysis) and inhibit SDH, supported by molecular docking and enzyme activity assays. Importantly, acute oral toxicity to bees was low (LC50 > 500 mg/L), comparable to commercial fungicides. These results identify A1 and A2 as promising, bee-safe leads for next-generation SDHI fungicides.

Boyi Sun, Hui Wang, Dandan Wang et al. · Journal of Agricultural and... · 0 citations