Development of active center-directed plasmin and plasma kallikrein inhibitors and studies on the structure-inhibitory activity relationship

DOI: 10.1248/cpb.41.1079

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 1079 - 1090 (1993)

Update date:2022-08-04

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Authors:

Teno Teno

Wanaka Wanaka

Okada Okada

Taguchi Taguchi

Okamoto Okamoto

Hijikata-Okunomiya

Okamoto Okamoto

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Article abstract of DOI:10.1248/cpb.41.1079

The molecule of trans-4-aminomethylcyclohexanecarbonylphenylalanine 4- carboxymethylanilide (8), which is a potent and selective inhibitor of plasma kallikrein, can be divided into three parts (P₁, P₁ and P₂), each of which contains one of the rings. In order to study the role of each part in the manifestation of potent and selective inhibitory activity and the relationship between the structure and inhibitory activities toward plasmin, plasma kallikrein, urokinase and thrombin, each part was substituted with various other moieties to give many kinds of analogs and their inhibitory activities against the above enzymes were examined. Among them, trans-4- aminomethylcyclohexanecarbonyl-O-2-bromobenzyloxycarbonyltyrosine 4- acetylanilide (12) inhibited plasmin and plasma kallikrein with IC₅₀ values of 2.3 x 10^-7 M and 3.7 x 10^-7 M, and K(i) values of 1.2 x 10^-7 M and 1.3 x 10^-7 M, respectively.

Full text of DOI:10.1248/cpb.41.1079

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