Anthranilamide inhibitors of factor Xa

…, T Goodson, JJ Masters, JB Franciskovich…

Index: Mendel, David; Marquart, Angela L.; Joseph, Sajan; Waid, Philip; Yee, Ying K.; Tebbe, Anne Louise; Ratz, Andrew M.; Herron, David K.; Goodson, Theodore; Masters, John J.; Franciskovich, Jeffry B.; Tinsley, Jennifer M.; Wiley, Michael R.; Weir, Leonard C.; Kyle, Jeffrey A.; Klimkowski, Valentine J.; Smith, Gerald F.; Towner, Richard D.; Froelich, Larry L.; Buben, John; Craft, Trelia J. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 17 p. 4832 - 4836

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Citation Number: 18

Abstract

SAR about the B-ring of a series of N2-aroyl anthranilamide factor Xa (fXa) inhibitors is described. B-ring o-aminoalkylether and B-ring p-amine probes of the S1′ and S4 sites, respectively, afforded picomolar fXa inhibitors that performed well in in vitro anticoagulation assays.