Fibrinogen Receptor (GPIIb-IIIa) Antagonists Derived from 5, 6-Bicyclic Templates. Amidinoindoles, Amidinoindazoles, and Amidinobenzofurans Containing the N-α- …

…, KJ Ruterbories, DJ Sall, RM Scarborough

Index: Su, Ting; Naughton, Mary Ann H.; Smyth, Mark S.; Rose, Jack W.; Arfsten, Ann E.; McCowan, Jefferson R.; Jakubowski, Joseph A.; Wyss, Virginia L.; Ruterbories, Kenneth J.; Sall, Daniel J.; Scarborough, Robert M. Journal of Medicinal Chemistry, 1997 , vol. 40, # 26 p. 4308 - 4318

Full Text: HTML

Citation Number: 33

Abstract

A series of highly potent and specific fibrinogen receptor antagonists have been discovered and optimized through structural modification of the novel amidinoindole and benzofuran compounds, I and II. Systematic linker optimization afforded the amidinobenzofuran- containing inhibitor 29, which displayed an IC50 value of 250 nM in platelet aggregation assays. Attempts to enhance activity by modification of the β-position of the β-alanyl ...