Solid-phase synthesis of amidine-based GP IIb-IIIa antagonists on dendrimer resin beads
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 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.
solid-phase organic synthesis, dendrimers, amidines, ro44-9883
fibrinogen receptor antagonists, peptide-synthesis, inhibitors, derivatives, reagent, design
3887-3891
Basso, A.
9cdcd616-ad0c-431a-b3f3-f39343a63694
Pegg, N.
864f9e25-f82f-4220-8694-6f6c8f820dc5
Evans, B.
4c435ee0-5ec3-4369-a9fc-f649824f98eb
Bradley, M.
078a34d6-96c4-4ce1-9aa1-454d9ee0030d
1 December 2000
Basso, A.
9cdcd616-ad0c-431a-b3f3-f39343a63694
Pegg, N.
864f9e25-f82f-4220-8694-6f6c8f820dc5
Evans, B.
4c435ee0-5ec3-4369-a9fc-f649824f98eb
Bradley, M.
078a34d6-96c4-4ce1-9aa1-454d9ee0030d
Abstract
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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Published date: 1 December 2000
Keywords:
solid-phase organic synthesis, dendrimers, amidines, ro44-9883
fibrinogen receptor antagonists, peptide-synthesis, inhibitors, derivatives, reagent, design
Identifiers
Local EPrints ID: 18911
URI: http://eprints.soton.ac.uk/id/eprint/18911
ISSN: 1434-193X
PURE UUID: f815b411-fab8-45a1-a7b2-1d5157cad3ad
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Date deposited: 17 Jan 2006
Last modified: 15 Mar 2024 06:09
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Author:
A. Basso
Author:
N. Pegg
Author:
B. Evans
Author:
M. Bradley
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