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Development of plasma kallikrein selective inhibitors

โœ Scribed by Yoshio Okada; Yuko Tsuda; Mayako Tada; Keiko Wanaka; Akiko Hijikata-Okunomiya; Utako Okamoto; Shosuke Okamoto

Publisher
Wiley (John Wiley & Sons)
Year
1999
Tongue
English
Weight
340 KB
Volume
51
Category
Article
ISSN
0006-3525

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โœฆ Synopsis

During the course of the development of active center-directed plasmin inhibitors, it was found that N-(trans-4-aminomethylcyclohexanecarbonyl)-lysine-4-methoxycarbonylanilide inhibited plasma kallikrein more potently than other enzymes such as plasmin, urokinase, and thrombin, although the inhibitory activity was not as potent and enzyme selectivity not as high. Based on studies of structure-activity relationship, we designed and synthesized the plasma kallikrein selective inhibitor, N-(trans-4-aminomethylcyclohexanecarbonyl)-phenylalanine-4-carboxymethyl-

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