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Design, Synthesis, and Structure-Activity Relationship of Quinazolinone Derivatives as Potential Fungicides

文献类型： 外文期刊

作者： Peng, Jing-Wen 1 ; Yin, Xiao-Dan 1 ; Li, Hu 1 ; Ma, Kun-Yuan 1 ; Zhang, Zhi-Jun 1 ; Zhou, Rui 1 ; Wang, Yu-Ling 2 ; Hu, G 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： phytopathogenic fungi; quinazolinone; Sclerotinia sclerotiorum

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：4.192； 五年影响因子：4.289 ）

ISSN： 0021-8561

年卷期： 2021 年 69 卷 16 期

页码：

收录情况： SCI

摘要： Plant diseases caused by phytopathogenic fungi reduce the yield and quality of crops. To develop novel antifungal agents, we designed and synthesized eight series of quinazolinone derivatives and evaluated their anti-phytopathogenic fungal activity. The bioassay results revealed that compounds KZL-15, KZL-22, 5b, 6b, 6c, 8e, and 8f exhibited remarkable antifungal activity in vitro. Especially, compound 6c displayed the highest bioactivity against Sclerotinia sclerotiorum, Pellicularia sasakii, Fusarium graminearum, and Fusarium oxysporum, displaying appreciable IC50 values (50% inhibitory concentration) of 2.46, 2.94, 6.03, and 11.9 mu g/mL, respectively. A further mechanism interrogation revealed abnormal mycelia, damaged organelles, and changed permeability of cell membranes in S. sclerotiorum treated with compound 6c. In addition, the in vivo bioassay indicated that compound 6c possessed comparable curative and protective effects (87.3 and 90.7%, respectively) to the positive control azoxystrobin (89.5 and 91.2%, respectively) at 100 mu g/mL concentration against S. sclerotiorum. This work validated the potential of compound 6c as a new and promising fungicide candidate, contributing to the exploration of potent antifungal agents.

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