☆ 4.7 Article

5-Piperazinyl-3-sulfonylindazoles as Potent and Selective 5-Hydroxytryptamine-6 Antagonists

JOURNAL OF MEDICINAL CHEMISTRY (2010)

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JOURNAL OF MEDICINAL CHEMISTRY

卷 53, 期 21, 页码 7639-7646

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AMER CHEMICAL SOC

DOI: 10.1021/jm1007825

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Chemistry, Medicinal

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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, SA R, and pharmacokinetic and pharmacological activities of some of the compounds including 3-(naphthalen-1-ylsulfonyl)-5-(piperazin-l-yl)-1H-indazole (WAY-255315 or SAM-315) will be described.

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