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Synthesis and Biological Evaluation of Biphenyl Amides That Modulate the US28 Receptor
Author(s) -
Kralj Ana,
Kurt Elif,
Tschammer Nuska,
Heinrich Markus R.
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201300369
Subject(s) - pharmacophore , moiety , biphenyl , allosteric regulation , chemistry , inverse agonist , agonist , combinatorial chemistry , stereochemistry , biological activity , receptor , organic chemistry , biochemistry , in vitro
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.