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ID: ALA1131988

Journal: Bioorg Med Chem Lett

Title: Synthesis, SAR and in vivo activity of novel thienopyridine sulfonamide pyrrolidinones as factor Xa inhibitors.

Authors: Becker MR, Ewing WR, Davis RS, Pauls HW, Ly C, Li A, Mason HJ, Choi-Sledeski YM, Spada AP, Chu V, Brown KD, Colussi DJ, Leadley RJ, Bentley R, Bostwick J, Kasiewski C, Morgan S.

Abstract: Thienopyridine sulfonamide pyrrolidinones were found to be potent and selective inhibitors of the coagulation cascade enzyme factor Xa. SAR studies led to several compounds that were selected for further in vivo investigation. These novel aryl binding pocket moieties represent a structural modification to a series of fXa inhibitors. Several compounds proved to be efficacious i.v. antithrombotic agents.

CiteXplore: 10509929

DOI: 10.1016/s0960-894x(99)00466-7