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Bioorg Med Chem Lett. 2004 Aug 16;14(16):4197-201.

Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.

Author information

1
Aventis Pharma Deutschland GmbH, D-65926 Frankfurt am Main, Germany. marc.navarre@aventis.com

Abstract

A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for P4 ligands in combination with a neutral biaryl P1 ligand were investigated with the 2-carboxyindole scaffold. A diverse set of P4 substituents was identified, which, in conjunction with a biaryl P1 ligand, gave highly potent factor Xa inhibitors, which were also selective versus other proteases and efficacious in various antithrombotic secondary assays.

PMID:
15261269
DOI:
10.1016/j.bmcl.2004.06.019
[Indexed for MEDLINE]

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