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- W2137469923 abstract "Structure-based drug design coupled with polymer-assisted solution-phase library synthesis was utilized to develop a series of pyrazinone inhibitors of the tissue factor/Factor VIIa complex. The crystal structure of a tri-peptide ketothiazole complexed with TF/VIIa was utilized in a docking experiment that identified a benzyl-substituted pyrazinone as a P(2) surrogate for the tri-peptide. A 5-step PASP library synthesis of these aryl-substituted pyrazinones was developed. The sequence allows for attachment of a variety of P(1) and P(3) moieties, which led to synthesis pyrazinone 23. Compound 23 exhibited 16 nM IC(50) against TF/VIIa with >6250x selectivity versus Factor Xa and thrombin. This potent and highly selective inhibitor of TF/VIIa was chosen for pre-clinical intravenous proof-of-concept studies to demonstrate the separation between antithrombotic efficacy and bleeding side effects in a primate model of thrombosis." @default.
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- W2137469923 date "2003-07-01" @default.
- W2137469923 modified "2023-09-26" @default.
- W2137469923 title "Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue factor VIIa complex" @default.
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- W2137469923 doi "https://doi.org/10.1016/s0960-894x(03)00410-4" @default.
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