Synthesis and Biological Evaluation of Biphenyl Amides That Modulate the US28 Receptor
CHEMMEDCHEM, cilt.9, sa.1, ss.151-168, 2014 (SCI-Expanded, Scopus)
- 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.