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- Charlotta Wallinder, Christian Sköld, Milad Botros, Marie-Odile Guimond, Mathias Hallberg, Nicole Gallo-Payet, Anders Karlén, and Mathias Alterman.
- Organic Pharmaceutical Chemistry, Department of Medicinal Chemistry, BMC, Uppsala University , SE-751 23 Uppsala, Sweden.
- Acs Med Chem Lett. 2015 Feb 12;6(2):178-82.
AbstractMigration 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.
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