Synthesis and Inhibition Effects on 5-HT6 Receptor of Benzothiazole Derivatives

Bulletin of the Korean chemical society

Hea-Young Park Choo¹  Hyewhon Rhim¹  Faisal Hayat¹  Euna Yoo¹ 

关键词: Sulfonamide;    N-Methyl piperazine;    5-HT6 receptor antagonist;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

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.

【 授权许可】

Unknown