1.
Bioorg Med Chem Lett
; 19(9): 2409-12, 2009 May 01.
Article
in English
| MEDLINE
| ID: mdl-19346128
ABSTRACT
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.
