Design, synthesis and biological evaluation of novel beta-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 better antioxidant than melatonin.
Iakovou
K
K
School of Pharmacy, Department of Pharmaceutical Chemistry, University of Athens, Panepistimiopolis-Zografou, Greece.
Varvaresou
A
A
Kourounakis
A P
AP
Stead
K
K
Sugden
D
D
Tsotinis
A
A
D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D007211:Indoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015227:Lipid Peroxidation / Q000187:drug effects*; D008550:Melatonin / Q000031:analogs & derivatives*; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D011916:Rats, Inbred F344; D011956:Receptors, Cell Surface / Q000187:drug effects; D018160:Receptors, Cytoplasmic and Nuclear / Q000187:drug effects; D044094:Receptors, Melatonin; D013329:Structure-Activity Relationship
D000975:Antioxidants; D007211:Indoles; D011956:Receptors, Cell Surface; D018160:Receptors, Cytoplasmic and Nuclear; D044094:Receptors, Melatonin; D008550:Melatonin