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  • Chem Sci Trans., 2019, 8(3),  pp 308-317  

    DOI:10.7598/cst2019.1455

    Research Article

    Design, Synthesis and Biological Evaluation of 3-n-Butylphthlide-Edaravone Hybrids as Potential Agents for the Treatment of Cerebral Ischemia

  • XIA-MIN HU1,2, WEI DONG1 , QIAN ZHANG1 , QIONG YUAN1, 3, 4, ZHI-WEN CUI1, CHENG-ZHI GAO1, ZHI-JUN YU1 and ZHEN-LI MIN1, 3, 4 *
  • 1 Department of Pharmacy, College of Medicine, Wuhan University of Science and Technology, Wuhan, Hubei Province 430065, China
    2 College of Pharmacy, Shanghai University of Medicine and Health Sciences, Shanghai 201318, China
    3 Drug Research Base of Cardiovascular and Cerebral Vascular, College of Medicine, Wuhan University of Science and Technology, Wuhan, Hubei Province 430065, China
    4 New Drugs Innovation and Development institute, Department of Pharmacy, College of Medicine, Wuhan University of Science and Technology, Wuhan, Hubei Province 430065, China
  • Abstract

    A series of 3-n-butylphthlide-edaravone hybrids was synthesized and their structures were elucidated on the basis of analytical and spectral (IR, 1H NMR, 13C NMR, MS and elemental analyses) data. These synthesized compounds were evaluated for their in vitro antiplatelet by the turbidimetric method and antioxidant activities by the Fenton method. The results indicated that compound 11a showed similar potency of antiplatelet aggregation as 3-n-butylphthlide and stronger ?OH scavenging activity (IC50 value of 2.87 mM) than edaravone (IC50 value of 3.57 mM).

    Keywords

    NBP, Edaravone, Antiplatelet, Antioxidant, Anti-cerebral ischemia

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