Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308

…, BP Damiano, P Andrade-Gordon…

文献索引：Hoekstra, William J.; Maryanoff, Bruce E.; Damiano, Bruce P.; Andrade-Gordon, Patricia; Cohen, Judith H.; Costanzo, Michael J.; Haertlein, Barbara J.; Hecker, Leonard R.; Hulshizer, Becky L.; Kauffman, Jack A.; Keane, Patricia; McComsey, David F.; Mitchell, John A.; Scott, Lorraine; Shah, Rekha D.; Yabut, Stephen C. Journal of Medicinal Chemistry, 1999 , vol. 42, # 25 p. 5254 - 5265

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被引用次数: 71

摘要

Although intravenously administered antiplatelet fibrinogen receptor (GPIIb/IIIa) antagonists have become established in the acute-care clinical setting for the prevention of thrombosis, orally administered drugs for chronic use are still under development. Herein, we present details from our exploration of structure-activity surrounding the prototype fibrinogen receptor antagonist RWJ-50042 (racemate of 1), which was derived from a unique ...