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ABSTRACT: A series of 5-HT(6) ligands derived from (R)-1-(amino)methyl-6-(phenyl)sulfonyltetralin was prepared that yielded several non-basic analogs having sub-nanomolar affinity. Ligand structure-activity relationships, receptor point mutation studies, and molecular modeling of these novel ligands all combined to reveal a new alternative binding mode to 5-HT(6) for antagonism.
Bioorganic & medicinal chemistry letters 06/2010; 20(11):3436-40. DOI:10.1016/j.bmcl.2010.03.110 · 2.42 Impact Factor