Mapping the melatonin receptor. 1. the 5-methoxyl group of melatonin is not an essential requirement for biological activity

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

A number of indole-derived melatonin analogues have been prepared lacking the C-5 methoxyl group. Many of these analogues are melatonin-receptor agonists and the previous assumption that the 5-OMe group was required for biological activity appears to have been an artefact mainly arising from the poor binding affinities of the small range of compounds tested.

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