Design, synthesis, and biological evaluation of pyrazinones containing novel P1 needles as inhibitors of TF/VIIa

John I. Trujillo,Horng-Chih Huang,William L. Neumann,Matthew W. Mahoney,Scott Long,Wei Huang,Danny J. Garland,Carrie Kusturin,Zaheer Abbas,Michael S. South,David B. Reitz

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

The design, synthesis, and biological evaluation of 20 compounds with novel P1 needles is reported. The P1 needle replacements were selected based upon their reduced basicity compared to the parent phenyl amidine (pKa∼12), with the goal of the effort an orally bioavailable TF/VIIa inhibitor.

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关键词

Factor VIIa,Anticoagulants,Thrombosis,Serine protease,Amidine,TF/VIIa,Antithrombotics,Oral,Pyrazinones

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