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

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

CHEMMEDCHEM, cilt.9, sa.1, ss.151-168, 2014 (SCI-Expanded, Scopus) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 9 Sayı: 1
  • Basım Tarihi: 2014
  • Doi Numarası: 10.1002/cmdc.201300369
  • Dergi Adı: CHEMMEDCHEM
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Index Chemicus (IC)
  • Sayfa Sayıları: ss.151-168
  • Acıbadem Mehmet Ali Aydınlar Üniversitesi Adresli: Hayır

Özet

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.