3 years ago

Microwave-assisted synthesis, characterization and bioassay of acylhydrazone derivatives as influenza neuraminidase inhibitors

Beibei Li, Jiao Ye, Mengwu Xiao, Aixi Hu, Ailin Liu, Wenwen Lian, Meng Zhang


A series of acylhydrazone derivatives (4a4s) were synthesized via microwave irradiation with short reaction time and good yields. The crystal structure of compound 4j was further determined by single-crystal X-ray diffraction. All of the derivatives were evaluated in vitro for influenza neuraminidase inhibitory activities. Among them, compounds 4l and 4n showed the most potent activity with IC50 values of 59.86 and 49.97 μM, respectively. Molecular docking was performed to study the interactions between the protein and compound 4n. The docking result revealed the potential dual-site binding model of the title compounds (“430 cavity-Linker-SA cavity” model) which provided a new idea for the design of novel influenza neuraminidase inhibitors.

Publisher URL: https://link.springer.com/article/10.1007/s00044-017-2015-6

DOI: 10.1007/s00044-017-2015-6

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