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1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor xa inhibitors. Part 3: Design, synthesis and sar of orally bioavailable benzamidine-P4 inhibitors
Using N,N-dialkylated benzamidines as the novel P4 motifs, we have designed and synthesized a class of 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent and selective fXa inhibitors with significantly improved hydrophilicity and in vitro anticoagulant activity. These benzamidine-P4 fXa inhibitors have displayed excellent oral bioavailability and long half-life.