ZHANG Lei, YAN Ding-an, TIAN Jin-ying, YE Fei, XIAO Zhi-yan. Design, synthesis and biological evaluation of amide derivatives as xanthine oxidase inhibitorsJ. Acta Pharmaceutica Sinica, 2017,52(6): 952-958. doi: 10.16438/j.0513-4870.2017-0251
Citation: ZHANG Lei, YAN Ding-an, TIAN Jin-ying, YE Fei, XIAO Zhi-yan. Design, synthesis and biological evaluation of amide derivatives as xanthine oxidase inhibitorsJ. Acta Pharmaceutica Sinica, 2017,52(6): 952-958. doi: 10.16438/j.0513-4870.2017-0251

Design, synthesis and biological evaluation of amide derivatives as xanthine oxidase inhibitors

  • Xanthine oxidase (XO) is a key enzyme in the synthesis of uric acid. Therefore, XO inhibitors play an important role in the antihyperuricemic therapy. Based on the template structures of febuxostat and topiroxostat, 18 amide derivatives were designed and synthesized. Among them, six showed apparent inhibitory activity against XO under the concentration of 10 μmol·L-1. Molecular docking revealed the possible interaction mode of this compound class, which may provide a clue for further molecular design.
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