| Autor: |
Liu KG; Wyeth Research, CN 8000, Princeton, New Jersey 08543, United States. liuk@lundbeck.com, Robichaud AJ, Bernotas RC, Yan Y, Lo JR, Zhang MY, Hughes ZA, Huselton C, Zhang GM, Zhang JY, Kowal DM, Smith DL, Schechter LE, Comery TA |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2010 Nov 11; Vol. 53 (21), pp. 7639-46. |
| DOI: |
10.1021/jm1007825 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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