Hu Yanhao, Xiong Zhengxi, Shaheen Hafiz Muhammad Usama, He Xu, Wei Mian, Chen Ping, Luo Xianghui, Yan Wei, Ye Yonghao, He Bo
State Key Laboratory of Agricultural and Forestry Biosecurity, College of Plant Protection, Nanjing Agricultural University, Nanjing 210095, PR China.
State & Local Joint Engineering Research Center of Green Pesticide Invention and Application, College of Plant Protection, Nanjing Agricultural University, Nanjing 210095, PR China.
J Agric Food Chem. 2025 Sep 24;73(38):23871-23880. doi: 10.1021/acs.jafc.5c04110. Epub 2025 Sep 15.
Rice sheath blight, caused by pathogen, poses a significant threat to global food security. To address this challenge, we designed and synthesized diphenyl ether hydrazone derivatives () as potential succinate dehydrogenase inhibitors. Most of these derivatives achieved 100% inhibition against at 50 μg/mL concentration. Notably, compound exhibited an exceptional efficacy of 95% control rate with an EC of 0.28 μg/mL, which significantly outperformed boscalid at a concentration of 200 μg/mL, without affecting the rice growth and development. Furthermore, after treatment with , the growth morphology and intracellular changes of mycelia were consistent with those observed with boscalid. Additionally, the IC values of compounds and were 1.55 and 1.11 μM, respectively, which were better than the IC value of boscalid (1.85 μM). The finding by molecular docking studies revealed that compound interacts with novel binding sites, offering an opportunity for the development of innovative SDH inhibitors for the efficient control of rice sheath blight disease.
由病原菌引起的水稻纹枯病对全球粮食安全构成重大威胁。为应对这一挑战,我们设计并合成了二苯醚腙衍生物()作为潜在的琥珀酸脱氢酶抑制剂。这些衍生物中的大多数在50μg/mL浓度下对[病原菌名称未给出]实现了100%的抑制。值得注意的是,化合物[具体化合物名称未给出]表现出95%的防治效果,有效浓度(EC)为0.28μg/mL,在200μg/mL浓度下显著优于啶酰菌胺,且不影响水稻的生长发育。此外,用[具体化合物名称未给出]处理后,[病原菌名称未给出]菌丝体的生长形态和细胞内变化与啶酰菌胺处理后的观察结果一致。另外,化合物[具体化合物名称未给出]和[具体化合物名称未给出]的半数抑制浓度(IC)值分别为1.55和1.11μM,优于啶酰菌胺的IC值(1.85μM)。分子对接研究结果表明,化合物[具体化合物名称未给出]与新的结合位点相互作用,为开发用于有效防治水稻纹枯病的新型琥珀酸脱氢酶抑制剂提供了契机。