Development of Plasmin-Selective Inhibitors and Studies of Their Structure-Activity Relationship

Yoshio OKADA; oshikazu MATSUMOTO; Yuko TSUDA; Mayako TADA; Keiko WANAKA; Akiko HIJIKATA-OKUNOMIYA; Shosuke OKAMOTO

doi:10.1248/cpb.48.184

Yoshio OKADA, oshikazu MATSUMOTO, Yuko TSUDA, Mayako TADA, Keiko WANAKA, Akiko HIJIKATA-OKUNOMIYA, Shosuke OKAMOTO

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Keywords: plasmin inhibitor, selectivity, structure-activity relationship, N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-BrZ)-octylamide

JOURNAL FREE ACCESS

2000 Volume 48 Issue 2 Pages 184-193

DOI https://doi.org/10.1248/cpb.48.184

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Abstract

Various compounds were synthesized by combining three components at positions P₁, P_1' and P_2'. Of these, N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-bromobenzyloxycarbonyl)-octylamide inhibited plasmin selectively with IC₅₀ values of 0.80 and 0.23 μM towards S-2251 and fibrin, respectively. THis compound also inhibited plasma kallikrein, urokinase, thrombin and trypsin with IC₅₀ values of 10, >50, >50 and 1.6 μM, rspectively.

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