209286-02-2Relevant academic research and scientific papers
Aminoisoquinolines: Design and synthesis of an orally active benzamidine isostere for the inhibition of factor Xa.
Choi-Sledeski,Becker,Green,Davis,Ewing,Mason,Ly,Spada,Liang,Cheney,Barton,Chu,Brown,Colussi,Bentley,Leadley,Dunwiddie,Pauls
, p. 2539 - 2544 (1999)
The design, synthesis and SAR of sulfonamidopyrrolidinone fXa inhibitors incorporating a new benzamidine isostere, namely aminoisoquinolines, is described. These inhibitors have higher Caco-2 cell permeability than comparable benzamidines and attain higher levels of exposure upon oral dosing. The most potent member 14b (fXa Ki=6 nM) is selective against other serine proteasesof interest (>600 fold).
