Novel and Potent 5-Piperazinyl Methyl-N1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands

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 comp...

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Veröffentlicht in:ACS medicinal chemistry letters 2010-10, Vol.1 (7), p.340-344
Hauptverfasser: Nirogi, Ramakrishna V. S., Kothmirkar, Prabhakar, Kambhampati, Ramasastri, Konda, Jagadish Babu, Arepalli, Sobhanadri, Pamuleti, Narasimhareddy G., Deshpande, Amol D., Bandyala, Trinathreddy, Shinde, Anil K., Dubey, P. K.
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Sprache:eng
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Zusammenfassung: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.
ISSN:1948-5875
1948-5875
DOI:10.1021/ml100101u