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  • Title: Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
    Author: Nazaré M, Essrich M, Will DW, Matter H, Ritter K, Urmann M, Bauer A, Schreuder H, Czech J, Lorenz M, Laux V, Wehner V.
    Journal: Bioorg Med Chem Lett; 2004 Aug 16; 14(16):4197-201. PubMed ID: 15261269.
    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.
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