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ID: ALA1149220
Journal: Bioorg Med Chem Lett
Title: 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.
Authors: Jia ZJ, Wu Y, Huang W, Zhang P, Clizbe LA, Goldman EA, Sinha U, Arfsten AE, Edwards ST, Alphonso M, Hutchaleelaha A, Scarborough RM, Zhu BY.
Abstract: A variety of P4 motifs have been examined to increase the binding affinity and in vitro anticoagulant potency of our biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamide-based fXa inhibitors. Highly potent 2-naphthyl-P1 fXa inhibitors (K(i)< or =2 nM) with improved in vitro anticoagulant activity (2xTG< or =1 microM) and respectable pharmacokinetic properties have been discovered.
CiteXplore: 14980670