Development of Potent and Selective Plasmin and Plasma Kallikrein Inhibitors and Studies on the Structure-Activity Relationship

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概要

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• Based on structure-activity relationship studies, we designed and synthesized plasmin (PL) and plasma Kallikrein (PK) inhibitors. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-Pic)-octylamide inhibited PL, PK, urokinase (UK) and thrombin (TH) with IC_<50> values of 0.53,30 5.3 and >400μM, respectively. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-Pyrim)-4-carboxyanilide inhibited PL, PK, UK and TH with IC_<50> values of 36,0.56,440 and >1000μM, respectively.

• 公益社団法人日本薬学会の論文
• 2000-12-01

著者

• TSUDA Yuko

  Faculty of Pharmaceutical Sciences, Kobe Gakuin University

• OKADA Yoshio

  Faculty of Pharmaceutical Sciences, Kobe Gakuin University

• Yokoi T

  Faculty Of Pharmaceutical Sciences Kobe Gakuin University

• Tsuda Yuko

  Faculty Of Pharmaceutical Sciences Kobe Gakuin University:cooperative Research Center Of Life Scienc

• Tsuda Yuko

  Faculty Of Pharmaceutical Science Kobe Gakuin University

• Okada Yoshio

  Faculty Of Pharmaceutical Sciences Kobe Gakuin University

• Hijikata-Okunomiya Akiko

  Faculty of Health Science, Kobe University School of Medicine

• Okamoto Shosuke

  Kobe Research Projects on Thrombosis and Haemostasis

• Takahashi M

  Research Center For Medicinal Plant Resources National Institute Of Biomedical Innovation

• TADA Mayako

  Faculty of Pharmaceutical Sciences, Kobe Gakuin University

• WANAKA Keiko

  Kobe Research Projects on Thrombosis and Haemostasis

• OKAMOTO Utako

  Kobe Research Projects on Thrombosis and Haemostasis

• Hijikata‐okunomiya A

  Faculty Of Health Science Kobe University School Of Medicine

• Hijikata-okunomiya Akiko

  Faculty Of Health Science Kobe University School Of Medicine

• Okamoto Shosuke

  Kobe Research Projects On Thrombosis And Haemostatis

• Wanaka Keiko

  Kobe Research Projects On Thrombosis And Haemostatis

• Okada Y

  Faculty Of Pharmaceutical Sciences Kobe Gakuin University

• Tada M

  Faculty Of Pharmaceutical Sciences Kobe Gakuin University

• Tsuda Y

  Faculty Of Pharmaceutical Sciences And High Technology Research Center Kobe Gakuin University

• 岡本 成羽

  Molecular Chemistry Laboratory Takeda Chemical Industries Ltd.

• Ogino Y

  Teikyo Univ. School Of Medicine Chiba

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