Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors
Bioorganic & Medicinal Chemistry Letters（2005）
Abstract
Reductive amination followed by acylation of polymer-linked formyl aryl amidines generate combinatorial libraries of aryl amidines. Potent small molecule naphthylamidine inhibitors (Ki<100nM) of FVIIa/TF have been discovered and their activity against other serine proteases in the coagulation cascade are reported.
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Key words
Solid-phase synthesis,Naphthylamidines,Factor VIIa/tissue factor inhibitors
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