Τίτλος:
Design, synthesis and biological evaluation of novel β-substituted indol-3-yl ethylamido melatoninergic analogues
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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.
Συγγραφείς:
Iakovou, K.
Varvaresou, A.
Kourounakis, A.P.
Stead, K.
Sugden, D.
Tsotinis, A.
Περιοδικό:
The Journal of pharmacy and pharmacology
Λέξεις-κλειδιά:
cyclobutanecarboxylic acid[2 (1 cyclobutanecarbonyl 1h indol 3 yl) 2 oxoethyl]amide; cyclobutanecarboxylic acid[2 (1 methyl 1h indol 3 yl) 2 oxoethyl]amide; cyclobutanecarboxylic acid[2 (1h indol 3 yl) 2 oxoethyl]amide; cyclobutanecarboxylic acid[2 hydroxy 2 (1 methyl 1h indol 3 yl)ethyl]amide; cyclopropanecarboxylic acid[2 (1 cyclopropanecarbonyl 1h indol 3 yl) 2 oxoethyl]amide; cyclopropanecarboxylic acid[2 (1 methyl 1h indol 3 yl) 2 oxoethyl]amide; cyclopropanecarboxylic acid[2 (1h indol 3 yl) 2 oxoethyl]amide; cyclopropanecarboxylic acid[2 hydroxy 2 (1 methyl 1h indol 3 yl)ethyl]amide; indole derivative; lipid; melatonin; melatonin derivative; melatonin receptor; n [2 (1 methyl 1h indol 3 yl) 2 oxoethyl]acetamide; n [2 (1 methyl 1h indol 3 yl) 2 oxoethyl]benzamide; n [2 (1 methyl 1h indol 3 yl) 2 oxoethyl]butyramide; n [2 (1 methyl 1h indol 3 yl) 2 oxoethyl]propionamide; n [2 (1h indol 3 yl) 2 oxoethyl]acetamide; n [2 (1h indol 3 yl) 2 oxoethyl]butyramide; n [2 (1h indol 3 yl) 2 oxoethyl]propionamide; n [2 hydroxy 2 (1 methyl 1h indol 3 yl)ethyl]acetamide; n [2 hydroxy 2 (1 methyl 1h indol 3 yl)ethyl]butyramide; n [2 hydroxy 2 (1 methyl 1h indol 3 yl)ethyl]propionamide; unclassified drug, agonist; animal cell; antioxidant activity; article; chemical modification; comparative study; concentration (parameters); controlled study; drug design; drug potency; drug receptor binding; drug screening; drug structure; drug synthesis; in vitro study; lipid peroxidation; liver microsome; melanophore; nonhuman; physical chemistry; rat; receptor affinity; structure activity relation; Xenopus, Animals; Antioxidants; Female; Indoles; Lipid Peroxidation; Melatonin; Microsomes, Liver; Rats; Rats, Inbred F344; Receptors, Cell Surface; Receptors, Cytoplasmic and Nuclear; Receptors, Melatonin; Structure-Activity Relationship
DOI:
10.1211/0022357021771869
