Document Report Card

ID: ALA3392997

Journal: ACS Med Chem Lett

Title: Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands.

Authors: Wallinder C, Sköld C, Botros M, Guimond MO, Hallberg M, Gallo-Payet N, Karlén A, Alterman M.

Abstract: Migration of the methylene imidazole side chain in the first reported selective drug-like AT2 receptor agonist C21/M024 (1) delivered the AT2 receptor antagonist C38/M132 (2). We now report that the AT2 receptor antagonist compound 4, a biphenyl derivative that is structurally related to 2, is transformed to the agonist 6 by migration of the isobutyl group. The importance of the relative position of the methylene imidazole and the isobutyl substituent is highlighted herein.

CiteXplore: 25699147

DOI: 10.1021/ml500427r