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. 2010 Nov 11;53(21):7639-46.
doi: 10.1021/jm1007825.

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

Kevin G Liu  1 , Albert J Robichaud, Ronald C Bernotas, Yinfa Yan, Jennifer R Lo, Mei-Yi Zhang, Zoe A Hughes, Christine Huselton, Guo Ming Zhang, Jean Y Zhang, Dianne M Kowal, Deborah L Smith, Lee E Schechter, Thomas A Comery
Affiliations

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

Kevin G Liu et al. J Med Chem. .

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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