Tramadol is an opioid prodrug that exhibits biological activity, along with its O-desmethyl metabolite.  The drug has a dual mechanism of action, and varied prescribed and off-label uses.  Its metabolite is a �-opioid receptor agonist, and tramadol itself inhibits the reuptake of serotonin and norepinephrine.  We are synthesizing a focused library of simplified analogs, based on tramadol by altering the amino, aryl, and hydroxyl positions.  The simplicity of the synthetic procedure will allow us to develop the preparation for the undergraduate organic chemistry laboratory. We will test the toxicity of our analogs in a brine shrimp bioassay that can be carried out by undergraduate biochemistry students.  The analogs that exhibit the least toxicity will be subjected to MTT assays, and those with promising activity will receive NCI 60 cancer screenings.

Drug discovery through simple analog synthesis and toxicity determination in the undergraduate laboratory experience

245th National Meeting (2013)

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