Aminoisoquinolines: design and synthesis of an orally active benzamidine isostere for the inhibition of factor XA.
1999
Abstract 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 proteases of interest (>600 fold).
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