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Discovery of novel flavonoid derivatives containing benzothiazole as potential antifungal agents
Pest Management Science ( IF 3.8 ) Pub Date : 2025-01-08 , DOI: 10.1002/ps.8632
Jiao Tian, Yi Liu, Hui Xin, Chunmei Hu, Jieyu Li, Yuhong Wang, Xingping Luo, Yujiao Qiu, Wei Xue
Pest Management Science ( IF 3.8 ) Pub Date : 2025-01-08 , DOI: 10.1002/ps.8632
Jiao Tian, Yi Liu, Hui Xin, Chunmei Hu, Jieyu Li, Yuhong Wang, Xingping Luo, Yujiao Qiu, Wei Xue
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BACKGROUNDFungal diseases of plants have a serious impact on the quality and yield of crops, and some traditional pesticides can no longer cope with this problem. Therefore, it is of great significance to develop new pesticides with high efficiency and low toxicity.RESULTSA series of flavonoid derivatives containing benzothiazole were designed and synthesized. Among them, the compounds V17, V12, and V13 had excellent inhibitory effect against Fusarium oxysporum f. sp. cucumerinu with the half‐maximal effect concentration (EC50 ) values of 1.2, 2.3, and 3.2 μg/mL, which were better than the control drug Kresoxim‐methyl (Km, 37.8 μg/mL). The in vivo protective activity and curative activities of V17 against cucumber fusarium wilt caused by F. oxysporum f. sp. cucumerinum were 82.4 and 60.5% at 200 μg/mL, better than Km (60.2 and 48.6%). In addition, V17 could damage the cell membrane of the mycelia, which can be confirmed by determination of cytoplasmic leakage, detection of cell membrane permeability, and measurement of malondialdehyde (MDA). Similarly, the scanning electron microscopy (SEM) experiment and optical microscope characterization provide direct evidence for destruction of mycelium treated with V17.CONCLUSIONV17 significantly reduced the pathogenicity of the F. oxysporum f. sp. cucumerinum , which provided a new idea and direction for the development of green pesticides. © 2025 Society of Chemical Industry.
中文翻译:
发现含有苯并噻唑作为潜在抗真菌剂的新型类黄酮衍生物
背景植物的真菌病害对农作物的品质和产量有严重影响,一些传统农药已经无法应对这一问题。因此,开发高效、低毒的新型农药具有重要意义。结果设计合成了一系列含苯并噻唑的类黄酮衍生物。其中,化合物 V17 、 V12 和 V13 对尖孢镰刀菌 (Fusarium oxysporum f. sp. cucumerinu) 具有优异的抑制效果,半数最大效应浓度 (EC50) 值为 1.2 、 2.3 和 3.2 μg/mL,优于对照药物甲基克雷索辛 (Km,37.8 μg/mL)。V17 对尖孢镰刀菌引起的黄瓜枯萎病的体内保护活性和疗效分别为 82.4% 和 60.5%,在 200 μg/mL 时优于 Km (60.2 和 48.6%)。此外,V17 可能会损害菌丝体的细胞膜,这可以通过测定细胞质渗漏、检测细胞膜通透性和丙二醛 (MDA) 来确认。同样,扫描电子显微镜 (SEM) 实验和光学显微镜表征为用 V17 处理的菌丝体的破坏提供了直接证据。CONCLUSIONV17显著降低了尖孢镰刀菌的致病性,为绿色农药的开发提供了新的思路和方向。© 2025 化工学会.
更新日期:2025-01-08
中文翻译:
![](https://scdn.x-mol.com/jcss/images/paperTranslation.png)
发现含有苯并噻唑作为潜在抗真菌剂的新型类黄酮衍生物
背景植物的真菌病害对农作物的品质和产量有严重影响,一些传统农药已经无法应对这一问题。因此,开发高效、低毒的新型农药具有重要意义。结果设计合成了一系列含苯并噻唑的类黄酮衍生物。其中,化合物 V17 、 V12 和 V13 对尖孢镰刀菌 (Fusarium oxysporum f. sp. cucumerinu) 具有优异的抑制效果,半数最大效应浓度 (EC50) 值为 1.2 、 2.3 和 3.2 μg/mL,优于对照药物甲基克雷索辛 (Km,37.8 μg/mL)。V17 对尖孢镰刀菌引起的黄瓜枯萎病的体内保护活性和疗效分别为 82.4% 和 60.5%,在 200 μg/mL 时优于 Km (60.2 和 48.6%)。此外,V17 可能会损害菌丝体的细胞膜,这可以通过测定细胞质渗漏、检测细胞膜通透性和丙二醛 (MDA) 来确认。同样,扫描电子显微镜 (SEM) 实验和光学显微镜表征为用 V17 处理的菌丝体的破坏提供了直接证据。CONCLUSIONV17显著降低了尖孢镰刀菌的致病性,为绿色农药的开发提供了新的思路和方向。© 2025 化工学会.