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  • Title: Development of potent and selective plasmin and plasma kallikrein inhibitors and studies on the structure-activity relationship.
    Author: Okada Y, Tsuda Y, Tada M, Wanaka K, Okamoto U, Hijikata-Okunomiya A, Okamoto S.
    Journal: Chem Pharm Bull (Tokyo); 2000 Dec; 48(12):1964-72. PubMed ID: 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.
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