Discovery of an orally active non-peptide fibrinogen receptor antagonist based on the hydantoin scaffold

…, O Klingler, W König, V Wehner, G Zoller

文献索引：Stilz; Guba; Jablonka; Just; Klingler; Koenig; Wehner; Zoller Journal of Medicinal Chemistry, 2001 , vol. 44, # 8 p. 1158 - 1176

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被引用次数: 72

摘要

Antagonists of the platelet fibrinogen receptor (GP IIb/IIIa receptor) are expected to be a promising new class of antithrombotic agents. The binding of fibrinogen to the fibrinogen receptor depends on an Arg-Gly-Asp-Ser (RGDS) tetrapeptide recognition motif. Structural modifications of the RGDS lead have led to the discovery of a non-peptide RGD mimetic GP IIb/IIIa antagonist 44 (S 1197). Compound 44 inhibited, in a dose dependent and ...