Design, Synthesis and Antifungal/Nematicidal Activity of Novel 1,2,4-Oxadiazole Derivatives Containing Amide Fragments.
Design, Synthesis and Antifungal/Nematicidal Activity of Novel 1,2,4-Oxadiazole Derivatives Containing Amide Fragments.
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DOI：
10.3390/ijms23031596
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发表时间：
2022-01-29
影响因子：
5.6
通讯作者：
Gan X
中科院分区：
文献类型：
--
作者：
Liu D;Luo L;Wang Z;Ma X;Gan X
近年来，由真菌和线虫引起的植物病害日益严重。然而，目前市场上可用于真菌和线虫联合防治的农药化学品还很少。为了解决这一问题，我们设计并合成了一系列新型的含有酰胺片段的1,2,4-恶二唑衍生物。此外，生物测定结果显示，化合物F15在体外对核盘菌（S. sclerotiorum）表现出优异的抗真菌活性，其EC50值为2.9 μg/mL，与常用杀菌剂噻氟酰胺和氟吡菌酰胺相当。同时，F15在体内对感染核盘菌的油菜表现出优异的治疗和保护活性。扫描电镜结果显示，F15处理后的菌核菌丝异常塌陷、皱缩，从而抑制了菌丝的生长。此外，F15对核盘菌的琥珀酸脱氢酶（SDH）表现出良好的抑制作用（IC50 = 12.5 μg/mL），并且通过分子对接证实了化合物F15与SDH的结合模式和结合能力。此外，化合物F11在200 μg/mL浓度下对南方根结线虫表现出优异的杀线虫活性，校正死亡率为93.2%，高于噻沙芬。
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 F15 demonstrated excellent antifungal activity against Sclerotinia sclerotiorum (S. sclerotiorum) in vitro, and the EC50 value of that was 2.9 μg/mL, which is comparable with commonly used fungicides thifluzamide and fluopyram. Meanwhile, F15 demonstrated excellent curative and protective activity against S. sclerotiorum-infected cole in vivo. The scanning electron microscopy results showed that the hyphae of S. sclerotiorum treated with F15 became abnormally collapsed and shriveled, thereby inhibiting the growth of the hyphae. Furthermore, F15 exhibited favorable inhibition against the succinate dehydrogenase (SDH) of the S. sclerotiorum (IC50 = 12.5 μg/mL), and the combination mode and binding ability between compound F15 and SDH were confirmed by molecular docking. In addition, compound F11 showed excellent nematicidal activity against Meloidogyne incognita at 200 μg/mL, the corrected mortality rate was 93.2%, which is higher than that of tioxazafen.
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