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. © 2007 Elsevier Ltd. All rights reserved.
Mendel, D., Marquart, A. L., Joseph, S., Waid, P., Yee, Y. K., Tebbe, A. L., … Craft, T. J. (2007). Anthranilamide inhibitors of factor Xa. Bioorganic and Medicinal Chemistry Letters, 17(17), 4832–4836. https://doi.org/10.1016/j.bmcl.2007.06.051