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ID: ALA1133371
Journal: Bioorg Med Chem Lett
Title: Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.
Authors: Gong Y, Pauls HW, Spada AP, Czekaj M, Liang G, Chu V, Colussi DJ, Brown KD, Gao J.
Abstract: The design, synthesis and SAR of amido-(propyl and allyl)-hydroxybenzamidine coagulation factor Xa inhibitors is described. These achiral inhibitors are selective for fXa vis a vis structurally related serine proteases and are readily prepared in 6-7 linear steps. The most potent member 9j (fXa Ki = 0.75 nM) is selective (>1000-fold) and an effective anticoagulant in mammalian plasma.
CiteXplore: 10698439