State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering/Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
School of Chemistry and Materials Science, Guizhou Education University, Wudang District, Guiyang 550018, China.
Int J Mol Sci. 2022 Jan 29;23(3):1596. doi: 10.3390/ijms23031596.
Plant diseases that are caused by fungi and nematodes have become increasingly serious in recent years. However, there are few pesticide chemicals that can be used for the joint control of fungi and nematodes on the market. To solve this problem, a series of novel 1,2,4-oxadiazole derivatives containing amide fragments were designed and synthesized. Additionally, the bioassays revealed that the compound demonstrated excellent antifungal activity against () in vitro, and the EC value of that was 2.9 μg/mL, which is comparable with commonly used fungicides thifluzamide and fluopyram. Meanwhile, demonstrated excellent curative and protective activity against -infected cole in vivo. The scanning electron microscopy results showed that the hyphae of treated with became abnormally collapsed and shriveled, thereby inhibiting the growth of the hyphae. Furthermore, exhibited favorable inhibition against the succinate dehydrogenase (SDH) of the (IC = 12.5 μg/mL), and the combination mode and binding ability between compound and SDH were confirmed by molecular docking. In addition, compound showed excellent nematicidal activity against at 200 μg/mL, the corrected mortality rate was 93.2%, which is higher than that of tioxazafen.
近年来，由真菌和线虫引起的植物病害变得越来越严重。然而，市场上可用于防治真菌和线虫的农药化学物质却很少。为了解决这个问题，设计并合成了一系列含有酰胺片段的新型 1,2,4-噁二唑衍生物。此外，生物测定结果表明，化合物 对 （）具有优异的体外抗真菌活性，EC 值为 2.9 μg/mL，与常用杀菌剂噻呋酰胺和氟吡菌胺相当。同时， 对 感染的 cole 具有优异的体内治疗和保护活性。扫描电子显微镜结果表明，用 处理的菌丝异常塌陷和枯萎，从而抑制了菌丝的生长。此外， 对 （SDH）表现出良好的抑制作用（IC = 12.5 μg/mL），并通过分子对接证实了化合物 和 SDH 之间的结合方式和结合能力。此外，化合物 在 200 μg/mL 时对 表现出优异的杀线虫活性，校正死亡率为 93.2%，高于噻唑菌胺。
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