5-Piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists

…, AJ Robichaud, RC Bernotas, Y Yan…

Index: Liu, Kevin G.; Robichaud, Albert J.; Bernotas, Ronald C.; Yan, Yinfa; Lo, Jennifer R.; Zhang, Mei-Yi; Hughes, Zoe A.; Huselton, Christine; Zhang, Guo Ming; Zhang, Jean Y.; Kowal, Dianne M.; Smith, Deborah L.; Schechter, Lee E.; Comery, Thomas A. Journal of Medicinal Chemistry, 2010 , vol. 53, # 21 p. 7639 - 7646

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Citation Number: 27

Abstract

As part of our efforts to develop agents for CNS diseases, we have been focused on the 5- HT6 receptor in order to identify potent and selective ligands for cognitive enhancement. Herein we report the identification of a novel series of 5-piperazinyl-3-sulfonylindazoles as potent and selective 5-HT6 antagonists. The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl ...