Inhibitory activity and mechanism of aryl furan thioesters containing 1,3,4-thiadiazole against Erwinia amylovora

文献类型： 外文期刊

第一作者： Wei, Junjie

作者： Wei, Junjie;Chen, Liangye;Li, Wanjun;Yi, Aoyun;Li, Wenlong;Cui, Zi-Ning;Shi, Yu;Wang, Xiangyun

作者机构：

关键词： Erwinia amylovora; pear fire blight; 1,3,4-thiadiazole; antibacterial activity; reactive oxygen species

期刊名称：PEST MANAGEMENT SCIENCE （ 影响因子：3.8； 五年影响因子：4.3 ）

ISSN： 1526-498X

年卷期： 2025 年

页码：

收录情况： SCI

摘要： BACKGROUNDThe Gram-negative bacterium Erwinia amylovora induces fire blight disease in Rosaceae hosts, severely damaging pome fruit trees including pear, apple, and hawthorn cultivars. Traditional control methods, such as antibiotics and copper-based agents, are associated with plant damage and the emergence of resistant bacterial strains, and present significant challenges. This study aims to design and synthesize a novel eco-friendly bactericide.RESULTSIn this study, we designed and synthesized 30 small-molecule compounds by combining 1,3,4-thiadiazole, a key moiety of zinc thiazole, with 5-phenyl-2-furan. Structural characterization of these compounds was performed using 1H and 13C NMR spectroscopy, complemented by elemental composition analysis. Compound II-10 was identified as the most promising compound in initial screenings, with a median effective concentration (EC50) of 9.04 mu g/mL. Inoculation experiments demonstrated that at a concentration of 200 mu g/mL, II-10 effectively inhibited E. amylovora and controlled pear fire blight, with its protective activity exceeding its curative effects. Furthermore, fluorescence microscopy, flow cytometry and scanning electron microscopy analysis revealed a potential mechanism of antimicrobial action involving reactive oxygen species generation, apoptosis and changes in bacterial morphology. Toxicity assessment showed that II-10 was non-toxic to zebrafish, earthworm and silkworm.CONCLUSIONThis study established that II-10 was a lead scaffold for the development to control pear fire blight, providing theoretical support for optimizing small-molecule compounds. (c) 2025 Society of Chemical Industry.

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