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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Veröffentlicht in:	Journal of pharmacy and pharmacology 2002-01, Vol.54 (1), p.147-156
Hauptverfasser:	Iakovou, K., Varvaresou, A., Kourounakis, A. P., Stead, K., Sugden, D., Tsotinis, A.
Format:	Artikel
Sprache:	eng
Schlagworte:	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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Zusammenfassung:	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