Author/Authors :
Rogier C. Buijsman، نويسنده , , Jan E. M. Basten، نويسنده , , Theo G. van Dinther، نويسنده , , Gijsbert A. van der Marel، نويسنده , , Constant A. A. van Boeckel، نويسنده , , Jacques H. van Boom، نويسنده ,
Abstract :
The synthesis of a novel antithrombotic consisting of a heparin pentasaccharide conjugated to the active site inhibitor (NAPAP) (i.e. compound I) is reported. This conjugate shows a unique pharmacological profile both in vitro and in vivo having direct anti-thrombin and ATIII-mediated anti-Xa activity. Furthermore, conjugate I has a prolonged in vivo half-life compared to NAPAP (1.5 h vs 9 min.).
