The β-carboline natural product eudistomin U binds to the 5-hydroxytryptamine receptor in the human brain. The 5-hydroxytryptamine receptor is a serotonergic receptor associated with the regulation of several neurological processes including mood, sleep, appetite, and anxiety. We have synthesized eudistomin U analogs with proposed binding affinity for this receptor. We will describe preliminary binding affinities of these molecules through the Psychoactive Drug Screening Program at the University of North Carolina. We will also describe their separation into enantiomeric atropisomers, followed by binding affinity experiments on each enantiomer. This work provides us with a more thorough characterization of the structure-function relationships between β-carbolines and the 5-hydroxytryptamine receptor.

Synthesis and atropisomeric binding of novel β-carbolines to brain receptors

253rd National Meeting (2017)

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