Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists

…, JJ Cook, CJ McIntyre, CA Hunt, RJ Gould…

Index: Askew, Benny C.; Bednar, Rodney A.; Bednar, Bohumil; Claremon, David A.; Cook, Jacquelynn J.; McIntyre, Charles J.; Hunt, Cecila A.; Gould, Robert J.; Lynch, Robert J.; Lynch Jr., Joseph J.; Gaul, Stanley L.; Stranieri, Maria T.; Sitko, Gary R.; Holahan, Marie A.; Glass, Joan D.; Hamill, Terrence; Gorham, Lynn M.; Prueksaritanont, Thomayant; Baldwin, John J.; Hartman, George D. Journal of Medicinal Chemistry, 1997 , vol. 40, # 12 p. 1779 - 1788

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Citation Number: 54

Abstract

The synthesis and pharmacological evaluation of 5 (L-738,167), a potent, selective non- peptide fibrinogen receptor antagonist is reported. Compound 5 inhibited the aggregation of human gel-filtered platelets with an IC50 value of 8 nM and was found to be> 33000-fold less effective at inhibiting the attachment of human endothelial cells to fibrinogen, fibronectin, and vitronectin than it was at inhibiting platelet aggregation. Ex vivo platelet ...