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

Bioorganic & medicinal chemistry letters 2004 Aug 16; 14(16):4191-5

Link to PubMed abstract

Nazaré M M, Essrich M M, Will D DW, Matter H H, Ritter K K, Urmann M M, Bauer A A, Schreuder H H, Dudda A A, Czech J J, Lorenz M M, Laux V V, Wehner V V

Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main, Germany. marc.nazare@aventis.com

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. This privileged fragment assembly approach yielded a set of equipotent, selective inhibitors with structurally diverse neutral P1 substituents.