Abstract
We review our work towards the design and synthesis of high-affinity melatonin ( N-acetyl-5-methoxytryptamine) agonist and antagonist compounds. High affinity melatonergic agonists were obtained by shifting the melatonin side chain from C 3 to N 1 of the indole ring system. Conversely, by moving the side chain from C 3 to C 2 it was possible to obtain melatonin antagonist compounds, albeit of moderate affinity.
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