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Inhibition of activated protein C by benzamidine derivatives
J Stürzebecher1, D Prasa, O Taby
1Institute of Pharmacology and Toxicology, Medical Academy Erfurt, Germany.
Thrombosis Research
|March 15, 1993
Abstract:
In studies on the inhibition of activated protein C (APC) by benzamidine derivatives potent inhibitors of APC were found among anilides of 4-amidinophenyl-alpha-aminobutyric acid (Ki = 0.58 mumol/l). Several bis-benzamidine derivatives containing a cycloalkanone linking bridge inhibit APC with Ki values near the micromolar range. Potent and selective inhibitors of thrombin derived from 3- and 4-amidinophenylalanine do not inhibit APC. This is of great importance for further development of these inhibitors as potential anticoagulant drugs.