Discovery of Aryloxy-, Arylthio-, and Arylamino-Containing Acethydrazides as Fungicidal Agents

• DOI: 10.1021/acs.jafc.2c06691
• Publication Date: 2022-12-19T21:25:57Z
• Authors: Hongbin Fang; Zhanfang Chen; Yang Liu; Tiancheng Zhang; Jing Chang; Zizheng Li; Lingxiao Zhang; Junkang Sui; Jing Ru; Yucheng Gu; Xuewen Hua
• Keywords: Organelle

The development of new green fungicides is an effective way to solve the resistance agricultural pathogens and plays important role in promoting high-quality sustainable modern agriculture. In this project, a series aryloxy-, arylthio-, arylamino-containing acethydrazide derivatives were designed, synthesized, characterized by 1H nuclear magnetic resonance (NMR), 13C NMR, high-resolution mass spectrometry (HRMS). fungicidal bioassays indicated that some compounds showed excellent broad-spectrum activity, structure-activity relationship was discussed. vivo activity demonstrated C4 D8 exhibited good preventative effects against Fusarium graminearum infecting wheat leaves, which compound almost equal positive agents. Transmission electron microscopy (TEM) observation revealed plasma membrane C4-treated F. hyphal cells severely contracted separated with cell wall, coupling visible lysosomes disappeared cytoplasm organelles, may be reasons for shriveled even ruptured hyphae observed scanning (SEM). Subsequently, transcriptomics metabolomics performed further elucidate mechanism. regulatory networks differential genes metabolites membrane-related sphingolipid metabolism, linoleic acid α-linoleic arachidonic metabolism constructed elaborated. Additionally, preliminary investigation seeding growth suggested have different degrees influence on indicators seedlings; however, effect negligible as plant grows.