Factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of neutral P1 substituents.

A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for neutral ligands, which bind in the S1 pocket of factor Xa were investigated with the 2-carboxyindole scaffold yielding a set of equipotent, selective inhibitors with structurally diverse neutral P1 substituents. The compound shown was found to be the most active in a number of antithrombotic secondary assays.