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ACS Med Chem Lett. 2010 Jun 24;1(7):340-4. doi: 10.1021/ml100101u. eCollection 2010 Oct 14.

Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.

Author information

1
Discovery Research, Suven Life Sciences Limited, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
2
Department of Chemistry, Jawaharlal Nehru Technological University Hyderabad.

Abstract

The exclusive distribution of 5-HT6 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-HT6R 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-HT6R; 5-Piperazinyl methyl-N1-aryl sulfonyl indole; Morris water mazes; NORT; PK profile; SAR

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