The exclusive distribution of 5-HT 6 receptors in the brain regions associated with learning and memory makes it an ideal target for cognitive disorders. A novel series of 5-piperazinyl methyl-N 1 -aryl sulfonyl indoles were designed and synthesized as 5-HT 6 R ligands. Most of the synthesized compounds are potent when tested by in vitro radioligand binding assay. The lead compound from the series does not have the CYP liabilities and is active in an animal model of cognition.KEYWORDS 5-Piperazinyl methyl-N 1 -aryl sulfonyl indole, 5-HT 6 R, NORT, SAR, Morris water mazes, PK profile T he 5-HT 6 receptors (5-HT 6 R) are perceived by the scientific community as possible targets for the treatment of cognitive disorders as well as obesity.
XVII), are prepared by facile methods and screened for in vitro biological activity. Moderate 5-HT6 receptor antagonist activities are found. -(NIROGI*, R. V. S.; KAMBHAMPATI, R. S.; KOTHMIRKAR, P.; AREPALLI, S.; PAMULETI, N. R. G.; SHIDE, A. K.; DUBEY, P. K.; Synth. Commun. 41 (2011) 19, 2835-2851, http://dx.
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