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ID: ALA1146956
Journal: Bioorg Med Chem Lett
Title: Factor VIIa inhibitors: a prodrug strategy to improve oral bioavailability.
Authors: Riggs JR, Kolesnikov A, Hendrix J, Young WB, Shrader WD, Vijaykumar D, Stephens R, Liu L, Pan L, Mordenti J, Green MJ, Sukbuntherng J.
Abstract: We have developed a series of potent and selective factor VIIa inhibitors based on the 2-[5-(5-carbamimidoyl-1H-benzoimidazol-2-yl)-6-hydroxy-biphenyl-3-yl]-succinic acid scaffold. These amidine-containing compounds have low oral bioavailability. Herein, we describe our efforts to improve the oral bioavailability of the parent amidine via a prodrug strategy where the amidine basicity and polarity were reduced with either an alkoxy-amidine or a carbamate prodrug.
CiteXplore: 16458507