Synthesis and pharmacological evaluation of aryl aminosulfonamide derivatives as potent 5-HT6 receptor antagonists

✍ Scribed by Ramakrishna V.S. Nirogi; Anand V. Daulatabad; G. Parandhama; Shaikh Mohammad; K.R. Sastri; Anil K. Shinde; P.K. Dubey

• Publisher: Elsevier Science
• Year: 2010
• Tongue: English
• Weight: 410 KB
• Volume: 20
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.06.060

✦ Synopsis

A series of novel aryl aminosulfonamides was designed and synthesized as 5-HT 6 receptor ligands. Many compounds screened in a functional reporter gene based assay displayed potent antagonistic activity with Kb values in the range of 0.02-10 nM. The lead compound 11m exemplified in this series showed good ADME surrogate properties, acceptable pharmacokinetic profile and is active in animal models of cognition like novel object recognition test and Morris water maze. The compound was selected for detailed profiling.