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

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.

SUBMITTER: Nirogi RV 

PROVIDER: S-EPMC4007800 | biostudies-other | 2010 Oct

REPOSITORIES: biostudies-other

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

Nirogi Ramakrishna V S RV   Kothmirkar Prabhakar P   Kambhampati Ramasastri R   Konda Jagadish Babu JB   Arepalli Sobhanadri S   Pamuleti Narasimhareddy G NG   Deshpande Amol D AD   Bandyala Trinathreddy T   Shinde Anil K AK   Dubey P K PK  

ACS medicinal chemistry letters 20100624 7

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. ...[more]