Inhibition of activated protein C by benzamidine derivatives.
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.
Institute of Pharmacology and Toxicology, Medical Academy Erfurt, Germany.
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Stürzebecher
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D
Prasa
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Taby
D001550:Benzamidines / Q000494:pharmacology*; D001777:Blood Coagulation / Q000187:drug effects; D007700:Kinetics; D010455:Peptides; D011486:Protein C / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013917:Thrombin / Q000037:antagonists & inhibitors
D001550:Benzamidines; D010455:Peptides; D011486:Protein C; D013917:Thrombin