1199795-12-4Relevant articles and documents
5-piperazinyl-3-sulfonylindazoles as potent and selective 5-hydroxytryptamine-6 antagonists
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.
experimental part, p. 7639 - 7646 (2011/02/21)
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.
