Cinnamylindoline 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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Abstract

A series of cinnamylindoline derivatives were synthesized, and their factor Xa (FXa) inhibitory activities and selectivity over trypsin were evaluated. Among them, some novel derivatives showed potent FXa inhibitory activities and good selectivity over trypsin. Especially, (E)-2-{5-[1-(acetimidoyl)piperidin-4-yloxy]-2-[2-(5-amidino-2-hydroxyphenyl)ethen-1-yl]indolin-1-ylsulfonyl}acetic acid (22f) having 2-hydroxycinnamyl moiety exhibited the most potent FXa inhibitory activity in vitro. Furthermore, 22f also exhibited potent anticoagulant activities in vitro.

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