Solid-phase synthesis of amidine-based GP IIb-IIIa antagonists on dendrimer resin beads

Many amidine-based molecules are known to be antagonists of the fibrinogen- GP IIb-IIIa interaction, therefore useful in the treatment of thrombotic de seases. Here we report the solid-phase synthesis of a small library of amid ines, starting from high-loading dendrimerised TentaGel beads, using resin- bound 4-amidinobenzoic acid as a template. These compounds mimic the struct ure of known active compounds like Lamifiban (Ro44-9883) and TAK-029; the f irst solid-phase synthesis of which is also reported in this paper.