Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 73, Issue -, Pages 217-224Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.12.014
Keywords
Antidepressant; Anticonvulsant; Quinolinone; Triazole; Forced swimming test; Maximal electroshock seizure
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Funding
- National Natural Science Foundation of China [81160382]
- National Science and Technology Major Project of China [2011ZX09102-003-03]
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A series of 1-substituted-6-(4H-1,2,4-triazol-4-yl)-3,4-dihydroquinolin-2(1H)-ones were designed, synthesized, and screened for their antidepressant and anticonvulsant activities. Interestingly, compounds 5i, 5j, 5m, and 5n led to significant reductions in the immobility time in the forced swimming test at a dose of 50 mg/kg, and exhibited higher levels of efficacy than the reference standard fluoxetine. In addition, compound Si exhibited greater efficacy than fluoxetine in the tail suspension test. The results of an open field test further confirmed that compound 5i provided a good antidepressant effect. In the maximal electroshock seizure screen, compounds 5c and 5d showed moderate levels of anticonvulsant. activity and protected 100% of the animals at a dose of 100 mg/kg. None of the synthesized compounds showed any neurotoxicity in the rotarod test at a dose of 100 mg/kg. (C) 2014 Elsevier Masson SAS. All rights reserved.
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