Design, synthesis and pharmacological evaluation of indolylsulfonamide amines as potent and selective 5-HT6 receptor antagonists
作者： Ramakrishna V. S. Nirogi , Thrinath Reddy Bandyala , Veena Reballi , Jagadishu Babu Konda , Anand V. Daulatabad
DOI: 10.3109/14756366.2014.889126
关键词: Lead compound 、 Reporter gene 、 Water maze 、 5-HT6 receptor 、 Stereochemistry 、 Chemistry 、 ADME 、 Receptor 、 Structure–activity relationship 、 Aryl
摘要: AbstractA series of N′-[3-(indole-1-sulfonyl) aryl]-N,N-dimethyl ethane-1,2-diamines and propane-1,3-diamines was designed synthesized as 5-HT6 receptor ligands. These compounds, when screened in a functional reporter gene-based assay, displayed potent antagonistic activity with Kb values the range 1.8–60 nM. The lead compound 9y has shown good ADME surrogate properties, acceptable pharmacokinetic profile is active animal models cognition like novel object recognition test Morris water maze. It selected for detailed profiling.
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