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Design and Discovery of Novel Antifungal Quinoline Derivatives with Acylhydrazide as a Promising Pharmacophore

文献类型： 外文期刊

作者： Yang, Yu-Dong 1 ; He, Ying-Hui 1 ; Ma, Kun-Yuan 1 ; Li, Hu 1 ; Zhang, Zhi-Jun 1 ; Sun, Yu 1 ; Wang, Yu-Ling 2 ; Hu, Guan- 1 ;

作者机构： 1.Lanzhou Univ, Sch Pharm, Lanzhou 730000, Peoples R China

2.Gansu Acad Agr Sci, Lanzhou 730000, Peoples R China

关键词： quinoline; acylhydrazine; oxadiazole; fungicidal activity; pathogenic fungi

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：5.279； 五年影响因子：5.269 ）

ISSN： 0021-8561

年卷期： 2021 年 69 卷 30 期

页码：

收录情况： SCI

摘要： Inspired by natural 2-quinolinecarboxylic acid derivatives, a series of quinoline compounds containing acylhydrazine, acylhydrazone, sulfonylhydrazine, oxadiazole, thiadiazole, or triazole moieties were synthesized and evaluated for their fungicidal activity. Most of these compounds exhibited excellent fungicidal activity in vitro. Significantly, compound 2e displayed the superior in vitro antifungal activity against Sclerotinia sclerotiorum, Rhizoctonia solani, Botrytis cinerea, and Fusarium graminearum with the EC50 values of 0.39, 0.46, 0.19, and 0.18 mu g/mL, respectively, and were more potent than those of carbendazim (EC50, 0.68, 0.14, >100, and 0.65 mu g/mL, respectively). Moreover, compound 2e could inhibit spore germination of F. graminearum. Preliminary mechanistic studies showed that compound 2e could cause abnormal morphology of cell walls and vacuoles, loss of mitochondrion, increases in membrane permeability, and release of cellular contents. These results indicate that compound 2e displayed superior fungicidal activities and could be a potential fungicidal candidate against plant fungal diseases.

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