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

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

Author information

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

Abstract

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
DOI:
10.1016/j.bmcl.2004.06.020
[Indexed for MEDLINE]

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