Synthesis of trans-4-Aminomethylcyclohexanecarbonyl-L- and -D-phenylalanine-4-carboxymethylanilide and Examination of Their Inhibitory Activity against Plasma Kallikrein

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概要

• 論文の詳細を見る

• Based on studies of structure-activity relationship, trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanine-4-carboxymethylanilide (Tra-Phe-APAA) was designed as a selective plasma kallikrein inhibitor and synthesized. Tra-Phe-APAA inhibited plasma kallikrein with a K_i value of 0.81 μM, while it inhibited glandular kallikrein, plasmin, urokinase, factor Xa and thrombin with K_i values of >500,390,200,>500,and >500 μM, respectively. However, its stereoisomer, Tra-D-Phe-APPA did not exhibit any detectable inhibitory activity against the above enzymes.

• 社団法人日本薬学会の論文
• 1992-07-25

著者

• 岡田 芳男

  Faculty of Pharmaceutical Sciences Kobe-Gakuin University

• 津田 裕子

  Faculty of Pharmaceutical Sciences

• 津田 裕子

  神戸学院大学薬学部薬品化学

• 岡田 芳男

  神戸学院大学 薬学部

• 和中 敬子

  Kobe Research Projects on Thrombosis and Haemostasis

• 岡本 歌子

  Kobe Research Projects on Thrombosis and Haemostasis

• 岡本 彰祐

  Kobe Research Projects on Thrombosis and Haemostasis

• 岡宮 明子

  School of Allied Medical Sciences, Kobe University

• 岡宮 明子

  School Of Allied Medical Sciences Kobe University

• 岡本 歌子

  血栓止血研究神戸プロジェクト

• 岡本 彰祐

  血栓止血研究神戸プロジェクト

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