Bioorganic and Medicinal Chemistry Letters p. 2539 - 2544 (1999)
Update date:2022-08-03
Topics:
Choi-Sledeski
Becker
Green
Davis
Ewing
Mason
Ly
Spada
Liang
Cheney
Barton
Chu
Brown
Colussi
Bentley
Leadley
Dunwiddie
Pauls
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).
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