Design, Synthesis, and Biological Activity of Novel Aromatic Amide Derivatives Containing Sulfide and Sulfone Substructures

• DOI: 10.1016/j.eng.2019.09.011
• Publication Date: 2020-03-24T23:54:17Z
• Authors: Xuewen Hua; Nannan Liu; Sha Zhou; Leilei Zhang; Hao Yin; Guiqing Wang; Zhijin Fan; Yi Ma
• Keywords: Sulfone; Amide; Proton NMR

In recent years, the damage caused by soil nematodes has become increasingly serious; however, varieties and structures of nematicides available on market are deficient. Fluopyram, a succinate dehydrogenase inhibitor (SDHI) fungicide developed Bayer AG in Germany, been widely used prevention control due to its high efficiency novel mechanism action. this paper, two series target compounds were designed synthesized with nematicidal fungicidal fluopyram as molecular skeleton order introduce sulfide sulfone substructures. The identified characterized 1H nuclear magnetic resonance (NMR), 13C NMR, high-resolution mass spectrometer (HRMS). bioassays revealed that most showed excellent activities at 200 µg·mL−1 comparison fluopyram, while nematode mortality rate dropped sharply 100 µg·mL−1, except for I-11 II-6. terms activity, compound I-9 was discovered have an inhibitory rate, docking simulation performed can provide important guidance design exploration efficient lead compounds.