Anthranilamide inhibitors of factor Xa

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.

SAR about the B-ring of N2-aroyl anthranilamide 3e is described. B-ring o-aminoalkylethers and B-ring p-amine probes of the S1′ and S4 sites, respectively, afforded picomolar factor Xa and nanomolar factor IIa inhibitors that were potent in in vitro anticoagulation assays.Figure optionsDownload as PowerPoint slide