Institute of Pesticides, College of Agriculture, Yangtze University, Jingzhou, China.
Hubei Engineering Technology Center for Pest Forewarning and Management, College of Agriculture, Yangtze University, Jingzhou, China.
Pest Manag Sci. 2023 Oct;79(10):3439-3450. doi: 10.1002/ps.7481. Epub 2023 Apr 10.
Plant pathogenic fungal infections have become a severe threat to the yield and quality of agricultural products, and new green antifungal agents with high efficiency and low toxicity are needed. In this study, a series of thiasporine A derivatives containing phenylthiazole-1,3,4-oxadiazole thione (ketone) structures were designed and synthesized, and their antifungal activities against six invasive and highly destructive phytopathogenic fungi were evaluated.
The results found that all compounds showed moderate to potent antifungal activity against six phytopathogenic fungi, and most of the E series compounds showed remarkable antifungal activity against Sclerotinia sclerotiorum and Colletotrichum camelliaet. In particular, compounds E1-E5, E7, E8, E13, E14, E17, and E22 showed more significant antifungal activity against S. sclerotiorum, with half-maximal effective concentration (EC ) values of 0.22, 0.48, 0.56, 0.65, 0.51, 0.39, 0.60, 0.56, 0.60, 0.63, and 0.45 μg mL , respectively, which were superior to that of carbendazim (0.70 μg mL ). Further activity studies showed that compound E1 possessed superior curative activities against S. sclerotiorum in vivo and better inhibitory effects on sclerotia germination and the formation of S. sclerotiorum compared with those of carbendazim.
This study indicates that these thiasporine A derivatives containing phenylthiazole-1,3,4-oxadiazole thione structures might be used as antifungal agents against S. sclerotiorum. © 2023 Society of Chemical Industry.
植物病原真菌的感染已成为农产品产量和质量的严重威胁，需要高效低毒的新型绿色抗真菌剂。本研究设计并合成了一系列含苯并噻唑-1,3,4-噁二唑硫酮（酮）结构的硫色菌素 A 衍生物，并评估了它们对六种侵袭性和高破坏性植物病原真菌的抗真菌活性。
结果发现，所有化合物对六种植物病原真菌均表现出中等至较强的抗真菌活性，大多数 E 系列化合物对核盘菌和炭疽菌表现出显著的抗真菌活性。特别是化合物 E1-E5、E7、E8、E13、E14、E17 和 E22 对核盘菌表现出更显著的抗真菌活性，半数有效浓度（EC ）值分别为 0.22、0.48、0.56、0.65、0.51、0.39、0.60、0.56、0.60、0.63 和 0.45μg/mL，优于多菌灵（0.70μg/mL）。进一步的活性研究表明，化合物 E1 对核盘菌具有优越的体内治疗活性，并且对核盘菌孢子萌发和形成的抑制作用优于多菌灵。
本研究表明，这些含苯并噻唑-1,3,4-噁二唑硫酮结构的硫色菌素 A 衍生物可能可作为防治核盘菌的抗真菌剂。© 2023 英国化学学会。
