Non-Peptide Glycoprotein IIb/IIIa Antagonists. 11. Design and in Vivo Evaluation of 3, 4-Dihydro-1 (1 H)-isoquinolinone-Based Antagonists and Ethyl Ester Prodrugs

JH Hutchinson, JJ Cook, KM Brashear…

Index: Hutchinson, John H.; Cook, Jacquelynn J.; Brashear, Karen M.; Breslin, Michael J.; Glass, Joan D.; Gould, Robert J.; Halczenko, Wasyl; Holahan, Marie A.; Lynch, Robert J.; Sitko, Gary R.; Stranieri, Maria T.; Hartman, George D. Journal of Medicinal Chemistry, 1996 , vol. 39, # 23 p. 4583 - 4591

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Citation Number: 67

Abstract

The structure-activity relationship of a series of orally active glycoprotein IIb/IIIa antagonists containing a nitrogen heterocycle grafted onto a 3, 4-dihydro-1 (1 H)-isoquinolinone core is described. These compounds are structurally novel analogs of the progenitor compound 1 (L-734,217,[[3 (R)-[2-(piperidin-4-yl) ethyl]-2-oxopiperidinyl] acetyl]-3 (R)-methyl-β-alanine) in which the lactam chiral center has been removed. The 4-piperazinyl-and 4-piperidinyl- ...