1,4-Benzoxazine-3(4H)-ones as Potent Inhibitors of Platelet Aggregation : Design, Synthesis and Structure-Activity Relations

  • Liu Chang
    College of Pharmaceutical Sciences, Southwest University
  • Tan Jia-Lian
    College of Pharmaceutical Sciences, Southwest University
  • Xiao Si-Yu
    College of Pharmaceutical Sciences, Southwest University
  • Liao Jie-Feng
    College of Pharmaceutical Sciences, Southwest University
  • Zou Guang-Rong
    College of Pharmaceutical Sciences, Southwest University
  • Ai Xi-Xi
    College of Pharmaceutical Sciences, Southwest University
  • Chen Jian-Bin
    College of Pharmaceutical Sciences, Southwest University
  • Xiang Yi
    Fourth People’s Hospital of Sichuan Province
  • Yang Quan
    Fourth People’s Hospital of Sichuan Province
  • Zuo Hua
    College of Pharmaceutical Sciences, Southwest University

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  • 1,4-Benzoxazine-3(4<i>H</i>)-ones as Potent Inhibitors of Platelet Aggregation: Design, Synthesis and Structure–Activity Relations

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A series of novel potentially platelet aggregation-inhibiting 1,4-benzoxazine-3(4H)-one derivatives was designed and synthesized through Smiles rearrangement, reduction and acetylation reactions. The antiaggregatory activities of the target molecules on arterial blood samples from rabbits, expressed by IC50 values (μM), were then evaluated in vitro against ADP induced platelet aggregation. The favorable IC50 values of compound 8c (IC50=8.99 µM) and 8d (IC50=8.94 µM) indicated that these two compounds were the most potent molecules among all the synthesized compounds. A detailed molecular docking study to explore the interaction of compounds 8c and 8d with GP IIb/IIIa receptor showed that they these two compounds were docked into the active site of GPIIb/IIIa receptor. These results suggest that the 1,4-benzoxazine-3(4H)-one derivatives are promising lead compounds to develop new platelet aggregation inhibitors.

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