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Inhibition of activated protein C by benzamidine derivatives |
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| Authors: | J. Stü rzebecher, D. Prasa,O. Taby |
| Affiliation: | a Institute of Pharmacology and Toxicology, Medical Academy Erfurt, D(O)-5010, Erfurt, Germany b Centre Nat. de Transfusion Sanguine, F-91943, Les Ulis, France |
| 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--aminobutyric acid (Ki = 0.58 μmol/1). 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. |
| Keywords: | Author Keywords: activated protein C benzamidines inhibition selective thrombin inhibitors |
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