Development of Active Center-Directed Plasmin and Plasma Kallikrein Inhibitors and Studies on the Structure-Inhibitory Activity Relationship

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概要

• 論文の詳細を見る

• The molecule of trans-4-aminomethylcyclohexanecarbonylphenylalanine 4-carboxymethylanilide (8), which is a potent and selective inhibitor of plasma kallikrein, can be devided into three parts (P_1,P_<1'> and P_<2'>), each of which contains one of the rings. In order to study the role of each part in the manifestation of potent and selective inhibitory activity and the relationship between the structure and inhibitory activities toward plasmin, plasma kallikrein, urokinase and thrombin, each part was substituted with various other moieties to give many kinds of analogs and their inhibitory activities against the above enzymes were examined. Among them, trans-4-aminomethylcyclohexanecarbonyl-O-2-bromobenzyloxycarbonyltyrosine 4-acetylanilide (12) inhibited plasmin and plasma kallikrein with IC_<50> values of 2.3×10^<-7> M and 3.7×10^<-7> M, and K_i values of 1.2×10^<-7> M and 1.3×10^<-7> M, respectively.

• 社団法人日本薬学会の論文
• 1993-06-15

著者

• 岡田 芳男

  Faculty of Pharmaceutical Sciences Kobe-Gakuin University

• 手納 直規

  Faculty of Pharmaceutical Sciences

• 岡田 芳男

  神戸学院大学 薬学部

• 田口 博明

  Faculty of Pharmaceutical Sciences, Kobe-Gakuin University

• 和中 敬子

  Kobe Research Projects on Thrombosis and Haemostasis

• 岡本 歌子

  Kobe Research Projects on Thrombosis and Haemostasis

• 奥宮 明子

  School of Allied Medical Sciences, Kobe University

• 岡本 彰祐

  Kobe Research Projects on Thrombosis and Haemostasis

• 手納 直規

  Faculty Of Pharmaceutical Sciences Kobe-gakuin University

• 岡本 歌子

  血栓止血研究神戸プロジェクト

• 田口 博明

  Faculty Of Pharmaceutical Sciences Kobe-gakuin University

• 岡本 彰祐

  血栓止血研究神戸プロジェクト

関連論文

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