Design, synthesis and biological evaluation of novel β-substituted indol-3-yl ethylamido melatoninergic analogues

A series of new melatonin analogues have been synthesized. Interestingly, two of the new compounds, 11c and 11e, which did not show any appreciable affinity for the melatonin receptor, were found to be potent inhibitors of lipid peroxidation in rat liver microsomes. Analogue 11c, in particular, is a...

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Bibliographic Details
Published in:Journal of pharmacy and pharmacology 2002-01, Vol.54 (1), p.147-156
Main Authors: Iakovou, K., Varvaresou, A., Kourounakis, A. P., Stead, K., Sugden, D., Tsotinis, A.
Format: Article
Language:English
Subjects:
Animals
Antioxidants - chemical synthesis
Antioxidants - chemistry
Antioxidants - pharmacology
Biological and medical sciences
Female
General and cellular metabolism. Vitamins
Indoles - chemical synthesis
Indoles - chemistry
Indoles - pharmacology
Lipid Peroxidation - drug effects
Medical sciences
Melatonin - analogs & derivatives
Microsomes, Liver - drug effects
Microsomes, Liver - metabolism
Pharmacology. Drug treatments
Rats
Rats, Inbred F344
Receptors, Cell Surface - drug effects
Receptors, Cytoplasmic and Nuclear - drug effects
Receptors, Melatonin
Structure-Activity Relationship
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Summary:A series of new melatonin analogues have been synthesized. Interestingly, two of the new compounds, 11c and 11e, which did not show any appreciable affinity for the melatonin receptor, were found to be potent inhibitors of lipid peroxidation in rat liver microsomes. Analogue 11c, in particular, is a better antioxidant than melatonin.
ISSN:0022-3573
2042-7158
DOI:10.1211/0022357021771869