Design and synthesis of melatonin receptors agonists and antagonists

We review our work towards the design and synthesis of high-affinity melato nin (N-acetyl-5-methoxytryptamine) agonist and antagonist compounds. High a ffinity 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 c ompounds, albeit of moderate affinity. (C) 2000 Elsevier Science S.A. All r ights reserved.