Development of plasmin-selective inhibitors and studies of their structure-activity relationship

DOI: 10.1248/cpb.48.184

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 184 - 193 (2000)

Update date:2022-09-26

Topics:

Authors:

Okada, Yoshio

Matsumoto, Yoshikazu

Tsuda, Yuko

Tada, Mayako

Wanaka, Keiko

Hijikata-Okunomiya, Akiko

Okamoto, Shosuke

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Article abstract of DOI:10.1248/cpb.48.184

Various compounds were synthesized by combining three components at positions P₁, P₁, and P₂,. 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, respectively.

Full text of DOI:10.1248/cpb.48.184

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