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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Authors | Kevin G Liu, 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 |
Journal | Journal of medicinal chemistry
(J Med Chem)
Vol. 53
Issue 21
Pg. 7639-46
(Nov 11 2010)
ISSN: 1520-4804 [Electronic] United States |
PMID | 20932009
(Publication Type: Journal Article)
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Chemical References |
- 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-1-yl)-1H-indazole
- Indazoles
- Ligands
- Nootropic Agents
- Piperazines
- Receptors, Serotonin
- Serotonin Antagonists
- Sulfones
- serotonin 6 receptor
- Glutamic Acid
- Acetylcholine
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Topics |
- Acetylcholine
(metabolism)
- Animals
- Biological Availability
- Brain
(metabolism)
- Glutamic Acid
(metabolism)
- HeLa Cells
- Humans
- Indazoles
(chemical synthesis, pharmacokinetics, pharmacology)
- Ligands
- Nootropic Agents
(chemical synthesis, pharmacokinetics, pharmacology)
- Piperazines
(chemical synthesis, pharmacokinetics, pharmacology)
- Rats
- Receptors, Serotonin
(metabolism)
- Serotonin Antagonists
(chemical synthesis, pharmacokinetics, pharmacology)
- Structure-Activity Relationship
- Sulfones
(chemical synthesis, pharmacokinetics, pharmacology)
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