Design and Synthesis of 3-[1-oxo-(4-aryl-1-piperazinyl)alkyl]-N- (arylsulfonyl)-indoles as Potential Antagonists Agents on 5- HT6 Receptors

Design and Synthesis of 3-[1-oxo-(4-aryl-1-piperazinyl)alkyl]-N- (arylsulfonyl)-indoles as Potential Antagonists Agents on 5- HT6 Receptors

Recabarren-Gajardo, G.; Espinosa-Bustos, C.; Hebel, D.; Meza, W.; Tapia, F.; Zárate, A.; Lagos, C.F.; Pessoa-Mahana, C.D.

Abstract:

The 5-HT6 receptor is the most recently identified and cloned member of the serotonin receptor family. Extensive research has shown that this receptor is expressed in brain regions known to be associated with learning and memory. Blockade of the 5-HT6 receptor function has shown to specifically increase cholinergic and glutamatergic neurotransmission, improving cognition parameters in a number of rodent behavioral models. Given the fundamental role of both the acetylcholine and glutamate systems in cognitive processes, and their disturbance in memory dysfunction, 5-HT6 receptors inhibitors may play a therapeutic role on the modulation of normal and/or dysfunctional memory. In this work we report the synthesis of a new series of N-(arylsulfonyl)- indoles compounds, targeted to 5-HT6 receptor.

The 5-HT6 receptor is the most recently identified and cloned member of the serotonin receptor family. Extensive research has shown that this receptor is expressed in brain regions known to be associated with learning and memory. Blockade of the 5-HT6 receptor function has shown to specifically increase cholinergic and glutamatergic neurotransmission, improving cognition parameters in a number of rodent behavioral models. Given the fundamental role of both the acetylcholine and glutamate systems in cognitive processes, and their disturbance in memory dysfunction, 5-HT6 receptors inhibitors may play a therapeutic role on the modulation of normal and/or dysfunctional memory. In this work we report the synthesis of a new series of N-(arylsulfonyl)- indoles compounds, targeted to 5-HT6 receptor.

Palavras-chave:

DOI: 10.5151/chempro-14bmos-R0169-2

Referências bibliográficas

• [1] 1 Liu, K.G. and Robichaud, A. J. Int. Rev. Neurobiol. 2010, 94, 1.
• [2] 2 López-Rodríguez, M. L. et al. J. Med. Chem. 2005, 48, 4216.

Como citar:

Recabarren-Gajardo, G.; Espinosa-Bustos, C.; Hebel, D.; Meza, W.; Tapia, F.; Zárate, A.; Lagos, C.F.; Pessoa-Mahana, C.D.; "Design and Synthesis of 3-[1-oxo-(4-aryl-1-piperazinyl)alkyl]-N- (arylsulfonyl)-indoles as Potential Antagonists Agents on 5- HT6 Receptors", p-169-169. In: In Blucher Chemistry Proceedings, São Paulo, v. 1, n. 1, Setembro.2013. São Paulo: Blucher, 2013.
ISSN 23184043, DOI 10.5151/chempro-14bmos-R0169-2