17607-01-1Relevant articles and documents
Synthesis and biological evaluation of biphenyl amides that modulate the US28 receptor
Kralj, Ana,Kurt, Elif,Tschammer, Nuska,Heinrich, Markus R.
, p. 151 - 168 (2014)
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. Hit HCMV GPCRs ASAP! Employing a straightforward synthetic access involving radical arylation, 38 new potential US28 allosteric modulators were prepared and biologically evaluated. The investigation of structure-activity relationships among the new biphenyl-derived ligands led to a consistent model and the discovery of four promising candidates with full inverse agonist properties. Copyright