884502-54-9Relevant academic research and scientific papers
Factor VIIa inhibitors: A prodrug strategy to improve oral bioavailability
Riggs, Jennifer R.,Kolesnikov, Aleksandr,Hendrix, John,Young, Wendy B.,Shrader, William D.,Vijaykumar, Dange,Stephens, Robin,Liu, Liang,Pan, Lin,Mordenti, Joyce,Green, Michael J.,Sukbuntherng, Juthamas
, p. 2224 - 2228 (2007/10/03)
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.
