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The Design, Synthesis, And Biological Evaluation Of Aplysinopsin Analogs As Potential Neuromodulators, Kevin Lewellyn
The Design, Synthesis, And Biological Evaluation Of Aplysinopsin Analogs As Potential Neuromodulators, Kevin Lewellyn
Electronic Theses and Dissertations
Aplysinopsins are tryptophan-derived natural products that have been isolated from a variety of marine organisms and have been shown to possess a range of biological activities. Initial synthesis of a library of 50 aplysinopsin analogs revealed that of the 12 serotonin receptor subtypes and 34 other CNS receptors, aplysinopsin analogs shoa high affinity for the 5-HT2B and 5-HT2C receptor subtypes, with selectivity for 5-HT2B over 5-HT2C. Bromination at C-4 and C-5 of the indole ring resulted in greater binding affinities, with Ki's as low as 35 nM. In addition, biological evaluation of the MAO-A and MAO-B inhibitory activities of these …