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

…, M Urmann, A Bauer, H Schreuder, A Dudda…

Index: Nazare, Marc; Essrich, Melanie; Will, David W.; Matter, Hans; Ritter, Kurt; Urmann, Matthias; Bauer, Armin; Schreuder, Herman; Dudda, Angela; Czech, Joerg; Lorenz, Martin; Laux, Volker; Wehner, Volkmar Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 16 p. 4191 - 4195

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Citation Number: 15

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.