Synthesis of oligomeric assemblies of a platelet-binding key disaccharide in heparin and their biological activities

Heparin, highly sulfated glycosaminoglycan, binds to platelets. A key disac charide unit in heparin was previously found to be responsible for the bind ing, and the Frequency of the disaccharide unit was important for the bindi ng potency. A newly developed method based on the reductive amination was e ffectively applied to prepare structurally defined oligomeric assemblies po ssessing multiple units of the key disaccharide. From their platelet-bindin g activities measured by the competitive binding assay, the enhancement of the activity was clearly observed with increasing number of the key disacch aride. (C) 2001 Elsevier Science Ltd. All rights reserved.