Synthesis and Biological Evaluation of Biphenyl Amides That Modulate the US28 Receptor

Kralj A., Kurt E., Tschammer N., Heinrich M. R.

CHEMMEDCHEM, vol.9, no.1, pp.151-168, 2014 (SCI-Expanded, Scopus) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 9 Issue: 1
  • Publication Date: 2014
  • Doi Number: 10.1002/cmdc.201300369
  • Journal Name: CHEMMEDCHEM
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Page Numbers: pp.151-168
  • Acibadem Mehmet Ali Aydinlar University Affiliated: No

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.