Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives

Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight ( M W: 335–391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions. Amidino-phenox...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2003-07, Vol.13 (14), p.2291-2295
Hauptverfasser:	Ries, Uwe J., Priepke, Henning W.M., Hauel, Norbert H., Haaksma, Eric E.J., Stassen, Jean M., Wienen, Wolfgang, Nar, Herbert
Format:	Artikel
Sprache:	eng
Schlagworte:	Amidines - chemical synthesis Amidines - pharmacology Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Chemical Phenomena Chemistry, Physical Crystallography, X-Ray Drug Design Fibrinolysin - antagonists & inhibitors Fibrinolytic Agents - chemical synthesis Fibrinolytic Agents - pharmacology Heterocyclic Compounds - chemical synthesis Heterocyclic Compounds - pharmacology Humans In Vitro Techniques Indicators and Reagents Medical sciences Models, Molecular Molecular Weight Partial Thromboplastin Time Pharmacology. Drug treatments Quinolines - chemical synthesis Quinolines - pharmacology Thrombin - antagonists & inhibitors Trypsin Inhibitors - chemical synthesis Trypsin Inhibitors - pharmacology
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Zusammenfassung:	Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight ( M W: 335–391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions. Amidino-phenoxy quinoline derivatives represent a new class of potent thrombin inhibitors with good selectivity and remarkably low molecular weight (MW: 335–391). X-ray analyses of thrombin-bound inhibitors revealed that enzyme inhibition is mainly based on hydrophobic interactions.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(03)00442-6