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Bioorg Med Chem Lett. 2004 Jun 7;14(11):2801-5.

Novel factor Xa inhibitors based on a benzoic acid scaffold and incorporating a neutral P1 ligand.

Author information

1
Aventis Pharma Deutschland GmbH, D-65926 Frankfurt, Germany.

Abstract

A series of novel, highly potent, achiral factor Xa inhibitors based on a benzoic acid scaffold and containing a chlorophenethyl moiety directed towards the protease S1 pocket is described. A number of structural features, such as the requirements of the P1, P4 and ester-binding pocket ligands were explored with respect to inhibition of factor Xa. Compound 46 was found to be the most potent compound in a series of antithrombotic secondary assays.

PMID:
15125936
DOI:
10.1016/j.bmcl.2004.03.059
[Indexed for MEDLINE]

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