Synthetic heparin-like antithrombotics

After the discovery of a unique pentasaccharide domain in heparin that is responsible for activation of antithrombin 111, many analogues have been synthesised which stimulate the inhibition of factor Xa. Some aspects of the synthesis of heparin like pentasaccharides are presented. Furthermore, pentasaccharide conjugates could be designed and synthesised which stimulate the antithrombin I11 mediated inhibition of both factor Xa and thrombin. INTRODUCTION Heparin (l), is an anticoagulant drug composed of a mixture of glycosaminoglycans (GAGS) purified from biological sources such as intestinal mucosa. The antithrombotic action of heparin mainly results from interactions with the protease inhibitor antithrombin I11 (AT-III), the heparidAT-I11 complex inactivates the blood coagulation factors Xa and thrombin.