Periodical
Design, Synthesis, and Antifungal Evaluation of Novel Cuminic Acid Derivatives as Potential Laccase Inhibitors
| العنوان: | Design, Synthesis, and Antifungal Evaluation of Novel Cuminic Acid Derivatives as Potential Laccase Inhibitors |
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| المؤلفون: | Yang, Zihui, Qiu, Yigui, Jin, Daojun, Zheng, Yiming, Cui, Zhennan, Li, Jia, Gu, Wen |
| المصدر: | Journal of Agricultural and Food Chemistry; December 2024, Vol. 72 Issue: 50 p27726-27736, 11p |
| مستخلص: | In search of novel natural product-based fungicides, 49 cuminic acid derivatives were designed, synthesized, and screened for their in vitro antifungal effects toward seven phytopathogenic fungi and oomycetes. Consequently, several derivatives exhibited strong antifungal activities toward Fusarium graminearum, Botryosphaeria dothidea, and Valsa mali. Among them, compound 2bexhibited the most potent antifungal activity toward B. dothidea(EC50= 0.96 mg/L), more powerful than chlorothalonil. The in vivo assay against B. dothideafound that the protective and curative effects of 2bwere comparable to chlorothalonil. Meanwhile, SEM and TEM observations indicated that 2bcould ruin the integrity of mycelial morphology and organelles of B. dothidea. Preliminary mechanism research showed that 2bincreased the cell membrane permeability and intracellular ROS level, as well as conspicuously decreased the mycelial dry weight and cell wall chitin contents of B. dothidea. The phytotoxicity test revealed that 2bshowed good safety on seeds of mung bean and radish. The in vitro laccase inhibitory activity assay and molecular docking study demonstrated that 2bcould be a promising laccase inhibitor. This type of cuminic acid hydrazide derivative would provide valuable inspiration for developing novel fungicides against B. dothidea. |
| قاعدة البيانات: | Supplemental Index |
| تدمد: | 00218561 15205118 |
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| DOI: | 10.1021/acs.jafc.4c04437 |