No abstract

A series of N 0 -[3-(indole-1-sulfonyl) aryl]-N,N-dimethyl ethane-1,2-diamines and N 0 -[3-(indole-1-sulfonyl) aryl]-N,N-dimethyl propane-1,3-diamines was designed and synthesized as 5-HT 6 receptor ligands. These compounds, when screened in a functional reporter gene-based assay, displayed potent antagonistic activity with K b values in the range of 1.8-60 nM. The lead compound 9y has shown good ADME surrogate properties, acceptable pharmacokinetic profile and is active in animal models of cognition like novel object recognition test and Morris water maze. It was selected for detailed profiling.