Journal of Medicinal Chemistry p. 7639 - 7646 (2010)
Update date:2022-08-05
Topics:
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.
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)-5-(piperazin-1-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.
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