Design, Synthesis and Biological Evaluation of Novel 7-Mercaptocoumarin Derivatives as α<sub>1</sub>-Adrenoceptor Antagonists

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  • Xie Sai-Sai
    State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University
  • Wang Xiao-Bing
    State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University
  • Li Jiang-Yan
    State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University
  • Kong Ling-Yi
    State Key Laboratory of Natural Medicines, Department of Natural Medicinal Chemistry, China Pharmaceutical University

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  • Design, Synthesis and Biological Evaluation of Novel 7-Mercaptocoumarin Derivatives as α1-Adrenoceptor Antagonists

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Study on the pharmacophore model of α1-adrenoceptor (α1-AR) antagonists led to design a series of novel 7-mercaptocoumarin derivatives as α1-AR antagonists. All designed compounds have been synthesized and biologically evaluated. The results showed that most of them exhibited strong antagonistic activity. Especially compound 6 showed excellent activity, which was better than that of the reference compound prazosin. Structure–activity relationship studies revealed that small hydrophobic group at the terminal heterocyclic ring and ortho substituents on the phenyl ring of phenylpiperazine moiety were the essential structural factors for α1-AR antagonistic activity. The pharmacophore modeling studies further clarified their structural contributions to antagonistic activity and also demonstrated that 7-mercaptocoumarin moiety could be a useful scaffold for design of α1-AR antagonists.

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