Pest management science · 2025
Discovery of novel 4-sulfur-substituted pyrazol-5-yl-benzamide derivatives containing amide/hydrazide/ester moieties as potential succinate dehydrogenase inhibitors.
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Li Yantao, Mu Yuxin, Xiong Jun, Xu Dan, Liu Xili, Xu Gong
Аннотация
BACKGROUND: Succinate dehydrogenase inhibitor (SDHI) fungicides have been widely utilized in the combat of plant pathogenic fungi due to their potent, broad-spectrum antifungal activity and unique mode of action. In this study, a series of novel 4-sulfur-substituted pyrazol-5-yl-benzamide derivatives containing amide, hydrazide, or ester moieties were synthesized to develop innovative SDH inhibitors.
RESULTS: The bioassay studies indicated that several compounds exhibited potent in vitro fungicidal activity against various fungi. Particularly, compound 4d demonstrated broad-spectrum fungicidal efficacy, with EC50 values of 0.21, 0.95, 0.64, 1.33, and 0.66 mg L-1 against Valsa mali, Botrytis cinerea, Rhizoctonia solani, Fusarium graminearum, and Gaeumannomyces graminis, respectively. In vivo studies demonstrated that compound 4d effectively prevented V. mali infection in apples at 50 mg L-1, showing superior protective and curative effects (93.4% and 85.5%) compared to lead compound A27 (68.7% and 57.0%) and commercial fungicide fluxapyroxad (55.4% and 43.6%). Enzymatic inhibition assays and molecular docking analysis suggested that compound 4d could serve as a potential SDH inhibitor.
CONCLUSION: This study offers valuable insights for expanding the fungicidal spectrum of pyrazol-5-yl-benzamide derivatives and further developing them as novel SDH inhibitors. © 2025 Society of Chemical Industry.
RESULTS: The bioassay studies indicated that several compounds exhibited potent in vitro fungicidal activity against various fungi. Particularly, compound 4d demonstrated broad-spectrum fungicidal efficacy, with EC50 values of 0.21, 0.95, 0.64, 1.33, and 0.66 mg L-1 against Valsa mali, Botrytis cinerea, Rhizoctonia solani, Fusarium graminearum, and Gaeumannomyces graminis, respectively. In vivo studies demonstrated that compound 4d effectively prevented V. mali infection in apples at 50 mg L-1, showing superior protective and curative effects (93.4% and 85.5%) compared to lead compound A27 (68.7% and 57.0%) and commercial fungicide fluxapyroxad (55.4% and 43.6%). Enzymatic inhibition assays and molecular docking analysis suggested that compound 4d could serve as a potential SDH inhibitor.
CONCLUSION: This study offers valuable insights for expanding the fungicidal spectrum of pyrazol-5-yl-benzamide derivatives and further developing them as novel SDH inhibitors. © 2025 Society of Chemical Industry.