Cyanopeptide analogues: new lead structures for the design and synthesis of new thrombin inhibitors

This contribution deals with the structure-based design and syntheses of the new serine protease inhibitors RA-1001 and RA-1002, which are analogues of the blue-green algae derived cyanopeptide aeruginosin 98-B. Both compounds inhibit thrombin with Ki values of 5.6 microM and 8.7 microM, respectivel...

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Veröffentlicht in:	Pharmazie 2002-11, Vol.57 (11), p.729-732
Hauptverfasser:	RADAU, G, STÜRZEBECHER, J
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Cyanobacteria - chemistry Drug Design Fibrinolysin - chemical synthesis Fibrinolysin - pharmacology Humans In Vitro Techniques Indicators and Reagents Kinetics Magnetic Resonance Spectroscopy Medical sciences Oligopeptides - chemistry Oligopeptides - pharmacology Pharmacology. Drug treatments Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - pharmacology Spectrophotometry, Infrared Structure-Activity Relationship Thrombin - antagonists & inhibitors Trypsin Inhibitors - chemical synthesis Trypsin Inhibitors - pharmacology
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Beschreibung
Zusammenfassung:	This contribution deals with the structure-based design and syntheses of the new serine protease inhibitors RA-1001 and RA-1002, which are analogues of the blue-green algae derived cyanopeptide aeruginosin 98-B. Both compounds inhibit thrombin with Ki values of 5.6 microM and 8.7 microM, respectively.
ISSN:	0031-7144