Neutral inhibitors of the serine protease factor Xa

A neutral inhibitor of the serine protease factor Xa was identified via a high-throughput screen of a commercial library. The initial lead 1 demonstrated reversible and competitive inhibition kinetics for factor Xa and possessed a high degree of selectivity versus other related serine proteases. Ini...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2001-07, Vol.11 (14), p.1801-1804
Hauptverfasser:	SHRADER, William D, YOUNG, Wendy B, SPRENGELER, Paul A, SANGALANG, Joan C, ELROD, Kyle, CARR, Grant
Format:	Artikel
Sprache:	eng
Schlagworte:	Aniline Compounds - chemistry Aniline Compounds - isolation & purification Aniline Compounds - pharmacology Antithrombin III - chemical synthesis Antithrombin III - chemistry Antithrombin III - metabolism Antithrombin III - pharmacology Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Catalytic Domain - physiology Drug Evaluation, Preclinical Fibrinolysin - drug effects Humans Mass Screening Medical sciences Models, Molecular Monte Carlo Method Pharmacology. Drug treatments Protein Conformation Structure-Activity Relationship Thiophenes - chemistry Thiophenes - isolation & purification Thiophenes - pharmacology Thrombin - drug effects Trypsin - drug effects Urokinase-Type Plasminogen Activator - drug effects
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Beschreibung
Zusammenfassung:	A neutral inhibitor of the serine protease factor Xa was identified via a high-throughput screen of a commercial library. The initial lead 1 demonstrated reversible and competitive inhibition kinetics for factor Xa and possessed a high degree of selectivity versus other related serine proteases. Initial modeling efforts and the generation of a series of analogues of 1 are described.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(01)00312-2