Discovery of novel heterocyclic factor VIIa inhibitors

The structure activity relationships and binding mode of novel heterocyclic Factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2- b]pyridine scaffold. Structure–activity relationships...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 16; no. 8; pp. 2270 - 2273
Main Authors:	Rai, Roopa, Kolesnikov, Aleksandr, Sprengeler, Paul A., Torkelson, Steven, Ton, Tony, Katz, Bradley A., Yu, Christine, Hendrix, John, Shrader, William D., Stephens, Robin, Cabuslay, Ronnell, Sanford, Ellen, Young, Wendy B.
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 15-04-2006 Elsevier
Subjects:	5-aminopyrrolo[3,2- b]pyridine Aminopyridines - chemistry Aminopyridines - pharmacology Anticoagulant Binding Sites Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Crystallography, X-Ray Drug Design Factor VIIa Factor VIIa - antagonists & inhibitors Factor VIIa crystal structure Fibrinolytic Agents - chemical synthesis Fibrinolytic Agents - pharmacology fVIIa Heterocyclic Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - pharmacology Humans Inhibitor Medical sciences Pharmacology. Drug treatments Structure-Activity Relationship Thromboplastin - antagonists & inhibitors fVIIa Factor VIIa crystal structure 5-aminopyrrolo[3,2- b]pyridine Inhibitor Anticoagulant Heterocyclic Factor VIIa Serine endopeptidases Enzyme Enzyme inhibitor Inhibitor: fVIIa In vitro Peptidases Structure activity relation Biphenyl derivatives 5-aminopyrrolo[3,2-b]pyridine Binding mode Hydrolases Ureas Factor Vila crystal structure: Anticoagulant Chemical synthesis Coagulation Factor VIIa Crystalline structure
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Summary:	The structure activity relationships and binding mode of novel heterocyclic Factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2- b]pyridine scaffold. Structure–activity relationships and binding mode of novel heterocyclic factor VIIa inhibitors will be described. In these inhibitors, a highly basic 5-amidinoindole moiety has been successfully replaced with a less basic 5-aminopyrrolo[3,2- b]pyridine scaffold.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2006.01.017