Synthesis and inhibition effects on 5-HT6 receptor of benzothiazole derivatives

Abstract

A novel series of aryl sulfonylpiperazine derivatives (5-15) were synthesized as 5-HT6 ligands. In vitro assay was evaluated by measuring the 5-HT-induced Ca2+ increases using HeLa cell line expressing the cloned human 5-HT6 receptor, and the compound 13 showed potent 5-HT6 receptor antagonistic effect with IC50 value of 3.9 μM. Compound 13 also showed good selectivity on the 5-HT6 over 5-HT4 and 5-HT7 receptors.