SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling Original Research Article

Structure–activity relationships of a series of bis-arylic compounds, investigated as 5-HT7R ligands, are reported. The main structural modifications involved a central aryl moiety (phenyl, pyridine, diazine, triazine) and the nature and position of an amine-containing aliphatic chain. The affinity of the synthesized compounds (26 nM–10 μM) was systematically correlated with other previously reported series of bis-arylic ligands and rationalized by a ligand-based pharmacophore approach.