Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists

The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists is described. The additional conformational restriction offered by the bicyclic nucleus results in 20−400-fold increases in potency compar...

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Veröffentlicht in:	Journal of medicinal chemistry 1997-08, Vol.40 (18), p.2843-2857
Hauptverfasser:	Sall, Daniel J, Arfsten, Ann E, Bastian, Jolie A, Denney, Michael L, Harms, Cathy S, McCowan, Jefferson R, Morin, John M, Rose, Jack W, Scarborough, Robert M, Smyth, Mark S, Um, Suzane L, Utterback, Barbara G, Vasileff, Robert T, Wikel, James H, Wyss, Virginia L, Jakubowski, Joseph A
Format:	Artikel
Sprache:	eng
Schlagworte:	Arginine Benzamidines - chemical synthesis Benzamidines - chemistry Benzamidines - pharmacology Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Enzyme-Linked Immunosorbent Assay Fibrinogen - metabolism Humans Indicators and Reagents Medical sciences Models, Molecular Molecular Conformation Molecular Structure Pharmacology. Drug treatments Platelet Aggregation - drug effects Platelet Aggregation Inhibitors - chemical synthesis Platelet Aggregation Inhibitors - chemistry Platelet Aggregation Inhibitors - pharmacology Platelet Glycoprotein GPIIb-IIIa Complex - antagonists & inhibitors Structure-Activity Relationship
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