Abstract
Analysis of the structure-activity relationship between twenty-three indoleamines and melatonin, based on a specific in vivo fish bioassay, is described. The results clearly define that only halogenation at position 6 or extension of the acetyl side-chain to propionyl or butyryl is tolerated without a decrease in activity. Removal of the indole double bond however, only leads to a less than ten-fold loss of activity. The over-all relevance of the data in the development of a metabolically stable melatonin agonist is discussed.
Published Version
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