Peng Jing-Wen, Yin Xiao-Dan, Li Hu, Ma Kun-Yuan, Zhang Zhi-Jun, Zhou Rui, Wang Yu-Ling, Hu Guan-Fang, Liu Ying-Qian
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. 2021 Apr 28;69(16):4604-4614. doi: 10.1021/acs.jafc.0c05475. Epub 2021 Apr 19.
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 , , , , , , and exhibited remarkable antifungal activity . Especially, compound displayed the highest bioactivity against , , , and , displaying appreciable IC values (50% inhibitory concentration) of 2.46, 2.94, 6.03, and 11.9 μg/mL, respectively. A further mechanism interrogation revealed abnormal mycelia, damaged organelles, and changed permeability of cell membranes in treated with compound . In addition, the bioassay indicated that compound 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 μg/mL concentration against . This work validated the potential of compound as a new and promising fungicide candidate, contributing to the exploration of potent antifungal agents.
由植物病原真菌引起的植物病害会降低作物的产量和品质。为了开发新型抗真菌剂，我们设计并合成了八个系列的喹唑啉酮衍生物，并评估了它们对植物病原真菌的抗真菌活性。生物测定结果表明，化合物 、 、 、 、 、 和 表现出显著的抗真菌活性。特别是，化合物 对 、 、 和 表现出最高的生物活性，其半数抑制浓度（IC 值）分别为 2.46、2.94、6.03 和 11.9 μg/mL。进一步的机制研究表明，用化合物 处理后的 中，菌丝体异常、细胞器受损且细胞膜通透性改变。此外，生物测定表明，在 100 μg/mL 浓度下，化合物 对 的治疗和保护效果（分别为 87.3%和 90.7%）与阳性对照嘧菌酯（分别为 89.5%和 91.2%）相当。这项工作验证了化合物 作为一种新的有前景的杀菌剂候选物的潜力，为探索有效的抗真菌剂做出了贡献。
