A series of 3a-arylmethoxy-3�-aryltropane and piperidine derivatives have been found to be exhibit potent affinity (nM) for dopamine transporters (DAT) and serotonin transporters (SERT) in rat brain tissue, respectively. The aim of the present study is to synthesize and evaluate 4-aryl-4-arylmethoxy piperidine derivatives that would have affinity towards multiple transporters. We have synthesized a series of target compounds via a three step process from 4-Boc-piperidone. The binding affinity for DAT, SERT and nor epinephrine transporters (NET) has been determined in rat brain tissue. The synthetic details and results of this SAR study will be presented.

Synthesis and biological evaluation of 4-aryl-4-arylmethoxy piperidine analogs on monoamine transporters

246th National Meeting (2013)

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