Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp

MS Egbertson, CTC Chang, ME Duggan…

Index: Egbertson, Melissa S.; Chang, Charles T.-C.; Duggan, Mark E.; Gould, Robert J.; Halczenko, Wasyl; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2537 - 2551

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Citation Number: 192

Abstract

Inhibitors of platelet-fibrinogen binding offer an opportunity to interrupt the final, common pathway for platelet aggregation. Small molecule inhibitors of the platelet fibrinogen receptor GPIIbAIIa were prepared and evaluated for their ability to prevent platelet aggregation. Compound 23m (L-700,462/MK-383) inhibited in vitro platelet aggregation with an IC50 of 9 nM and demonstrated a selectivity of> 24 000-fold between platelet and human umbilical ...