ChemMedChem

Synthesis and biological evaluation of biphenyl amides that modulate the US28 receptor

A Kralj, E Kurt, N Tschammer, MR Heinrich

Index: Kralj, Ana; Kurt, Elif; Tschammer, Nuska; Heinrich, Markus R. ChemMedChem, 2014 , vol. 9, # 1 p. 151 - 168

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Citation Number: 13

Abstract

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 ...