THROMBIN INHIBITORS BASED ON THE AMINO ACID SEQUENCE OF HIRUDIN

摘要

A thrombin inhibitor comprising a first bulky hydrophobic portion interactin g with the catalytic sits of thrombin responsi- ble for proteolysis and a second portion at least maintaining the hydrophobi c and acidic character of amino acids 55 to 60 of na- tive hirudin at the C-terminal non-catalytic region of N-acetyl-hirudin45-65 . Between the first and second portions is a divalent linker moiety having a chain length of at least 10 carbon atomes. Preferably , the bulky hydrophobic portion comprises at least one amino acid of D-configuration. The compounds are useful in the treatment of thrombotic disorders.