Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors

[Display omitted] Heterocyclic amide isosteres were incorporated into a phenylglycine-based tissue factor/factor VIIa (TF–FVIIa) inhibitor chemotype, providing potent inhibitors. An X-ray co-crystal structure of phenylimidazole 19 suggested that an imidazole nitrogen atom effectively mimics an amide...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2015-05, Vol.25 (10), p.2169-2173
Hauptverfasser:	Glunz, Peter W., Cheng, Xuhong, Cheney, Daniel L., Weigelt, Carolyn A., Wei, Anzhi, Luettgen, Joseph M., Wong, Pancras C., Wexler, Ruth R., Priestley, E. Scott
Format:	Artikel
Sprache:	eng
Schlagworte:	Amide isosteres Crystallography, X-Ray Drug Design Factor VIIa Factor VIIa - antagonists & inhibitors Imidazoles - chemistry Molecular Structure Serine protease inhibitors Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology TF–FVIIa inhibitor Tissue factor
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