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  • Title: Synthesis and biological evaluation of biphenyl amides that modulate the US28 receptor.
    Author: Kralj A, Kurt E, Tschammer N, Heinrich MR.
    Journal: ChemMedChem; 2014 Jan; 9(1):151-68. PubMed ID: 24265151.
    Abstract:
    To prepare and biologically evaluate 38 new potential US28 allosteric modulators, we employed a straightforward synthetic route involving radical arylation. The study was based on a former lead structure but with the dihydroisoquinolinone moiety replaced by substituted biphenyls. The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a preliminary pharmacophore model and the discovery of four promising candidates with full inverse agonist properties.
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