Synthesis and Inhibition Effects on 5-HT₆Receptor 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 Ca 2+ 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.

Synthesis, Spectral Characterization and Antioxidant Activity of Novel Zafirlukast Sulfonyl Derivatives

“…3 Piperazinyl linked ciprofloxacin dimers reported as potent antibacterial agents against resistant strains. 4 Sulfonamide and substituted sulfonamide derivatives are important category of pharmacophores that have a wide spectrum of biological and pharmacological applications such as antimalarial, 5 antimicrobial, 6 antibacterial, 7,8 anticancer, 9 antifungal, 10 antihelmintic, 10 antioxidant, 11 antiHIV, 12 antitumor, 12 antiplasmodial, 13 antineoplastic, 14 antiproliferative 15 activities and additionally known to act as 5-HT 6 , 5-HT 7 receptor antagonists, 16,17 A2B and CXCR3 antagonists, 18,19 11b-HSD, 20 histone deacetylase (HDAC) inhibitors, 21 b-secretase (BACE1) inhibitors 22 and dual PI3K/mTOR inhibitors. 23 In recent years, literature reveals that the research interest and applications of antioxidants have constantly gathered high importance to eradicate the oxidative stress in humans.…”