5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists
Journal of Medicinal Chemistry2010Vol. 53(21), pp. 7639–7646
Citations Over TimeTop 22% of 2010 papers
Kevin G. Liu, Albert J. Robichaud, Ronald C. Bernotas, Yinfa Yan, Jennifer R. Lo, Meiyi Zhang, Zoë A. Hughes, Christine Huselton, Guo Ming Zhang, Jean Y. Zhang, Dianne Kowal, Deborah L. Smith, Lee E. Schechter, Thomas A. Comery
Abstract
As part of our efforts to develop agents for CNS diseases, we have been focused on the 5-HT(6) 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-HT(6) antagonists. The synthesis, SAR, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.
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