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

AbstractA series of acylhydrazone derivatives (4a–4s) were synthesized via microwave irradiation with short reaction time and good yields. The crystal structure of compound4j was further determined by single-crystal X-ray diffraction. All of the derivatives were evaluated in vitro for influenza neuraminidase inhibitory activities. Among them, compounds4l and4n 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 compound4n. 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.

Source: Medicinal Chemistry Research - November 7, 2017 Category: Chemistry Source Type: research