Author/Authors :
Benoit Bachand، نويسنده , , Micheline Tarazi، نويسنده , , Yves St-Denis، نويسنده , , Jeremy J. Edmunds، نويسنده , , Peter D. Winocour، نويسنده , , Lorraine Leblond، نويسنده , , M. Arshad Siddiqui، نويسنده ,
Abstract :
Bicyclic piperazinone based thrombin inhibitors of general structure 2 were prepared and evaluated in vitro and in vivo. These inhibitors, having in common an electrophilic basic trans-cyclohexylamine P1 residue, displayed high thrombin affinity, high selectivity against trypsin and good in vivo efficacy in the rat arterial thrombosis model.