Identification of orally bioavailable, non-amidine inhibitors of Urokinase Plasminogen Activator (uPA)

The discovery, synthesis, and early SAR work on a benzyl amine containing series of uPA inhibitors is reported. In this Letter we report the synthesis and evaluation of a series of non-amidine inhibitors of Urokinase Plasminogen Activator (uPA). Starting from compound 1, a significant change provide...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-10, Vol.19 (19), p.5712-5715
Hauptverfasser:	West, Christopher W., Adler, Marc, Arnaiz, Danny, Chen, Deborah, Chu, Kieu, Gualtieri, Giovanna, Ho, Elena, Huwe, Christoph, Light, David, Phillips, Gary, Pulk, Rebecca, Sukovich, Drew, Whitlow, Marc, Yuan, Shendong, Bryant, Judi
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Amidines - chemistry Analytical, structural and metabolic biochemistry Animals Benzylamines - chemistry Binding Sites Biological and medical sciences Crystallography, X-Ray Enzymes and enzyme inhibitors Fundamental and applied biological sciences. Psychology Humans Hydrolases Medical sciences Miscellaneous Pharmacology. Drug treatments Rats Serine protease Serine Proteinase Inhibitors - administration & dosage Serine Proteinase Inhibitors - chemical synthesis Serine Proteinase Inhibitors - chemistry Structure-Activity Relationship uPA Urokinase Urokinase-Type Plasminogen Activator - antagonists & inhibitors Urokinase-Type Plasminogen Activator - metabolism
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