Design, synthesis, and crystal structure of selective 2-pyridone tissue factor VIIa inhibitors
JJ Parlow, RG Kurumbail, RA Stegeman…
Index: Parlow, John J.; Kurumbail, Ravi G.; Stegeman, Roderick A.; Stevens, Anna M.; Stallings, William C.; South, Michael S. Journal of Medicinal Chemistry, 2003 , vol. 46, # 22 p. 4696 - 4701
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Citation Number: 62
Abstract
Targeted 2-pyridones were selected as tissue Factor VIIa inhibitors and prepared from 2, 6- dibromopyridine via a multistep synthesis. A variety of chemical transformations, including regioselective nucleophilic addition, selective nitrogen alkylation, and a Suzuki coupling, afforded the targeted tissue Factor VIIa inhibitors. The pyridone core was selected as a replacement for the pyrazinone core of noncovalent tissue Factor VIIa inhibitors and ...
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