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Solid‐Phase Synthesis of Amidine‐Based GP IIb‐IIIa Antagonists on Dendrimer Resin Beads
Author(s) -
Basso Andrea,
Pegg Neil,
Evans Brian,
Bradley Mark
Publication year - 2000
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/1099-0690(200012)2000:23<3887::aid-ejoc3887>3.0.co;2-t
Subject(s) - amidine , chemistry , solid phase synthesis , dendrimer , combinatorial chemistry , phase (matter) , stereochemistry , polymer chemistry , organic chemistry , biochemistry , peptide
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.