N-arylsulfonyl-2-vinyltryptamines as new 5-HT6 serotonin receptor Ligands

Abstract

Several new 2-vinyl-Nb, Nb-dimethyltryptamines were prepared using Fischer indole synthesis followed by simple functional group transformations and evaluated on 5-HT4, 5-HT5, 5-HT6 and 5-HT7 serotonin receptors. It was found that 2-vinyl substitution conferred a potent and selective 5-HT6 binding activity to these molecules which could be enhanced by Na-arylsulfonyl substituents. © 2006 Taylor & Francis.