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Development of potent and selective plasmin and plasma kallikrein inhibitors and studies on the structure-activity relationship.

作者信息

Okada Y, Tsuda Y, Tada M, Wanaka K, Okamoto U, 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 Dec;48(12):1964-72. doi: 10.1248/cpb.48.1964.

DOI:10.1248/cpb.48.1964
PMID:11145152
Abstract

Based on structure-activity relationship studies, we designed and synthesized plasmin (PL) and plasma kallikrein (PK) inhibitors. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-Pic)-octylamide inhibited PL, PK, urokinase (UK) and thrombin (TH) with IC50 values of 0.53, 30, 5.3 and > 400 microm, respectively. Trans-(4-aminomethylcyclohexanecarbonyl)-Tyr(O-2-Pyrim)-4-carboxyanilide inhibited PL, PK, UK and TH with IC50 values of 36, 0.56, 440 and > 1,000 microM, respectively.

摘要

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