Factor Xa inhibitors based on a 2-carboxyindole sc...[Bioorg Med Chem Lett. 2004]

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1: Bioorg Med Chem Lett. 2004 Aug 16;14(16):4191-5. Links

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

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

PMID: 15261268 [PubMed - indexed for MEDLINE]

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

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