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Bioorg Med Chem Lett
; 19(9): 2409-12, 2009 May 01.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19346128
RESUMEN
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.