See today's edition of
DailyUpdates in your
therapeutic area
Search all articles

Keywords:

Boolean terms AND, OR, NOT can be used. Phrases should be entered within quotes. For wildcards use an *

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

Bioorganic & medicinal chemistry letters 2004 Aug 16; 14(16):4197-201

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, Czech J J, Lorenz M M, Laux V V, Wehner V V

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

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.