From natural products to achiral drug prototypes: Potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs

A series of dihydropyrid-2-ones was synthesized and tested for inhibitory activity against serine protease enzymes. Moderate to low nanomolar inhibitory activities were obtained against thrombin and excellent selectivity against trypsin was observed.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (18), p.5429-5432
Hauptverfasser:	HANESSIAN, Stephen, THERRIEN, Eric, JIANBIN ZHANG, VAN OTTERLO, Willem, YAFENG XUE, GUSTAFSSON, David, NILSSON, Ingemar, FJELLSTRÖM, Ola
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Cattle Crystallography, X-Ray Humans Medical sciences Models, Molecular Pharmacology. Drug treatments Protein Binding Pyridones - chemical synthesis Pyridones - chemistry Pyridones - pharmacology Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology Thrombin - antagonists & inhibitors Thrombin - chemistry Thrombin - metabolism Trypsin - metabolism
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Beschreibung
Zusammenfassung:	A series of dihydropyrid-2-ones was synthesized and tested for inhibitory activity against serine protease enzymes. Moderate to low nanomolar inhibitory activities were obtained against thrombin and excellent selectivity against trypsin was observed.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.07.107