Development of plasmin-selective inhibitors and studies of their structure-activity relationship.
作者信息
Okada Y, Matsumoto Y, Tsuda Y, Tada M, Wanaka K, Hijikata-Okunomiya A, Okamoto S
机构信息
Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Japan.
出版信息
Chem Pharm Bull (Tokyo). 2000 Feb;48(2):184-93. doi: 10.1248/cpb.48.184.
PMID:10705502
Abstract
Various compounds were synthesized by combining three components at positions P1, P1' and P2'. Of these, N-(trans-4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-bromobenzylo xycarbonyl)- octylamide inhibited plasmin selectively with IC50 values of 0.80 and 0.23 microM 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 microM, respectively.
摘要
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