Cinnamyl Derivatives: Synthesis and Factor Xa (FXa) Inhibitory Activities

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  • Noguchi Tetsuji
    Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Tanaka Naoki
    Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
  • Nishimata Toyoki
    Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
  • Goto Riki
    Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.
  • Hayakawa Miho
    Medicinal Chemistry Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Sugidachi Atsuhiro
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Ogawa Taketoshi
    Biological Research Laboratories I, Daiichi Sankyo Co., Ltd.
  • Asai Fumitoshi
    Biological Research Laboratories II, Daiichi Sankyo Co., Ltd.
  • Fujimoto Koichi
    Medicinal Chemistry Research Laboratories I, Daiichi Sankyo Co., Ltd.

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To develop a potent and oral anticoagulant, a series of compounds with cinnamyl moiety was synthesized and their factor Xa (FXa) inhibitory activities were examined. As a result, some cinnamyl derivatives showed potent FXa inhibitory activities in vitro. Among them, compounds with substituent at the 3-position on the central benzene ring represented by (N-{4-[1-(acetimidoyl)piperidin-4-yloxy]-3-chlorophenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid dihydrochloride (45b) and (N-{4-[1-(acetimidoyl)piperidin-4-yloxy]-3-carbamoylphenyl}-N-[(E)-3-(3-amidinophenyl)-2-propenyl]sulfamoyl)acetic acid dihydrochloride (45j) exhibited potent FXa inhibitory activities with IC50 values of less than 10 nM in vitro. These compounds also showed potent anticoagulant activities both in vitro and ex vivo. Furthermore, these compounds exhibited no lethal toxicity (30 mg/kg, i.v.).

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