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Synthesis of trans-4-aminomethylcyclohexanecarbonyl-L- and -D-phenylalanine-4-carboxymethylanilide and examination of their inhibitory activity against plasma kallikrein.

作者信息

Wanaka K, Okada Y, Tsuda Y, Okamoto U, Hijikata-Okunomiya A, Okamoto S

机构信息

Kobe Research Projects on Thrombosis and Haemostasis, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Jul;40(7):1814-7. doi: 10.1248/cpb.40.1814.

DOI:10.1248/cpb.40.1814
PMID:1394697
Abstract

Based on studies of structure-activity relationship, trans-4-aminomethylcyclohexanecarbonyl-L-phenylalanine-4-carbox ymethylanilide (Tra-Phe-APAA) was designed as a selective plasma kallikrein inhibitor and synthesized. Tra-Phe-APAA inhibited plasma kallikrein with a Ki value of 0.81 microM, while it inhibited glandular kallikrein, plasmin, urokinase, factor Xa and thrombin with Ki values of greater than 500, 390, 200, greater than 500, and greater than 500 microM, respectively. However, its stereoisomer, Tra-D-Phe-APPA did not exhibit any detectable inhibitory activity against the above enzymes.

摘要

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