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

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

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...

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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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container_end_page 344
container_issue 7
container_start_page 340
container_title ACS medicinal chemistry letters
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creator 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
description 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.
doi_str_mv 10.1021/ml100101u
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title Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands
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