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

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概要

• 論文の詳細を見る

• 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.

• 公益社団法人日本薬学会の論文
• 2007-10-01

著者

• Tanaka N

  Department Of Pharmacology School Of Pharmaceutical Sciences Mukogawa Women's University

• Tanaka Naoko

  武庫川女子大学 薬学部薬理学

• Tanaka Naoki

  Medical ProteoScope Co., Ltd.

• 中西 務

  Faculty Of Pharmaceutical Sciences Setsunan University

• Tanaka N

  School Of Pharmaceutical Sciences Mukogawa Women S University

• Ogawa T

  R & D Division Daiichi Sankyo Co. Ltd.

• NOGUCHI Tetsuji

  Medicinal Chemistry Research Laboratories II, 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.

• Goto R

  R & D Division Daiichi Sankyo Co. Ltd.

• Hayakawa Miho

  R & D Division Daiichi Sankyo Co. Ltd.

• Asai Fumitoshi

  R & D Division Daiichi Sankyo Co. Ltd.

• Fujimoto K

  R & D Division Daiichi Sankyo Co. Ltd.

• Noguchi Tetsuji

  R & D Division Daiichi Sankyo Co. Ltd.

• Sugidachi Atsuhiro

  R & D Division Daiichi Sankyo Co. Ltd.

• Nishimata Toyoki

  R & D Division Daiichi Sankyo Co. Ltd.

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