Synthesis and SAR of tolylamine 5-HT 6 antagonists

The synthesis and SAR of tolylamines with 5-HT 6 receptor antagonist activity is presented. The amine, core aromatic, peripheral aromatic, and ether linker moieties of HTS hit 1 were modulated and the effect on potency at 5-HT 6 examined. Tolylpiperidine ether 9h was found to possess desirable pharm...

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Bibliographic Details
Published inBioorganic & medicinal chemistry letters Vol. 19; no. 9; pp. 2409 - 2412
Main Authors Singer, Jamie M., Wilson, Michael W., Johnson, Paul D., Graham, Shelley R., Cooke, Leonard W., Roof, Robin L., Boxer, Peter A., Gold, Lisa H., Meltzer, Leonard T., Janssen, Ann, Roush, Nicole, Campbell, Jeffrey E., Su, Ti-Zhi, Hurst, Susan I., Stoner, Chad L., Schwarz, Jacob B.
Format Journal Article
LanguageEnglish
Published Elsevier Ltd 2009
Subjects
5-HT6
Object recognition
Phenylpiperidine
5-HT6
Phenylpiperidine
Object recognition
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Summary:The synthesis and SAR of tolylamines with 5-HT 6 receptor antagonist activity is presented. The amine, core aromatic, peripheral aromatic, and ether linker moieties of HTS hit 1 were modulated and the effect on potency at 5-HT 6 examined. Tolylpiperidine ether 9h was found to possess desirable pharmacokinetic (PK) properties, and was also shown to enhance cognition in the rat novel object recognition paradigm.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2009.03.077