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

  • J Med Chem. 2010 Nov 11;53(21):7639-46. doi: 10.1021/jm1007825.
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
  • 1. Wyeth Research, CN 8000, Princeton, New Jersey 08543, United States. [email protected]
PMID: 20932009 DOI: 10.1021/jm1007825
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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