Basso, A., Pegg, N., Evans, B. and Bradley, M.
Solid-phase synthesis of amidine-based GP IIb-IIIa antagonists on dendrimer resin beads
European Journal of Organic Chemistry, (23), . (doi:10.1002/1099-0690(200012)2000:23<3887::AID-EJOC3887>3.0.CO;2-T).
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Many amidine-based molecules are known to be antagonists of the fibrinogen-GP IIb-IIIa interaction, therefore useful in the treatment of thrombotic deseases. Here we report the solid-phase synthesis of a small library of amidines, starting from high-loading dendrimerised TentaGel beads, using resin-bound 4-amidinobenzoic acid as a template. These compounds mimic the structure of known active compounds like Lamifiban (Ro44-9883) and TAK-029; the first solid-phase synthesis of which is also reported in this paper.
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