School of Pharmacy, Lanzhou University, Lanzhou 730000, People's Republic of China.
Gansu Academy of Agricultural Sciences, Lanzhou 730000, People's Republic of China.
J Agric Food Chem. 2020 Oct 7;68(40):11096-11104. doi: 10.1021/acs.jafc.0c01322. Epub 2020 Sep 28.
Phytopathogenic fungal infections have become a major threat to agricultural production, food security, and human health globally, and novel antifungal agents with simple chemical scaffolds and high efficiency are needed. In this study, we designed and synthesized 38 8-hydroxyquinoline metal complexes and evaluated their antifungal activities. The results showed that most of the tested compounds possessed remarkable antifungal activity. Especially, compound exhibited the highest antifungal potency among all target compounds, with EC values of 0.0940, 0.125, 2.95, and 5.96 μg/mL, respectively, against , , , and . Preliminary mechanistic studies had shown that compound might cause mycelial abnormalities of , cell membrane permeability changes, leakage of cell contents, and inhibition of sclerotia formation and germination. Moreover, the results of antifungal activity of compound against showed that possessed higher curative effects than that of the positive control azoxystrobin. Therefore, compound is expected to be a novel leading structure for the development of new antifungal agents.
植物病原真菌感染已成为全球农业生产、粮食安全和人类健康的主要威胁，需要具有简单化学结构和高效的新型抗真菌药物。在这项研究中，我们设计并合成了 38 种 8-羟基喹啉金属配合物，并评估了它们的抗真菌活性。结果表明，大多数测试的化合物具有显著的抗真菌活性。特别是化合物 表现出所有目标化合物中最高的抗真菌活力，对 、 、 、 的 EC 值分别为 0.0940、0.125、2.95 和 5.96μg/mL。初步的机制研究表明，化合物 可能导致 的菌丝异常、细胞膜通透性改变、细胞内容物泄漏以及抑制菌核形成和萌发。此外，化合物 对 的抗真菌活性结果表明，化合物 比阳性对照肟菌酯具有更高的治疗效果。因此，化合物 有望成为开发新型抗真菌药物的新型先导结构。
