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ID: ALA1147598
Journal: Bioorg Med Chem Lett
Title: 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 3: Design, synthesis and SAR of orally bioavailable benzamidine-P4 inhibitors.
Authors: Jia ZJ, Wu Y, Huang W, Zhang P, Song Y, Woolfrey J, Sinha U, Arfsten AE, Edwards ST, Hutchaleelaha A, Hollennbach SJ, Lambing JL, Scarborough RM, Zhu BY.
Abstract: 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.
CiteXplore: 14980671