Novel -Arylsulfonylindoles Targeted as Ligands of the 5-HT Receptor. Insights on the Influence of C-5 Substitution on Ligand Affinity.

A new series of twenty-two C-5 substituted -arylsulfonylindoles was prepared with the aim of exploring the influence of C-5 substitution on 5-HT receptor affinity. Eleven compounds showed moderate to high affinity at the receptor ( = 58-403 nM), with compound being identified as the most potent ligand. However, regarding C-5 substitution, both methoxy and fluorine were detrimental for receptor affinity compared to our previously published unsubstituted compounds.