Design, synthesis and evaluation of the antidepressant and anticonvulsant activities of triazole-containing quinolinones

• Derivatives of triazole-containing quinolinones were synthesized and screened for antidepressant and anticonvulsant activity.
• Compounds 5i, 5j, 5m, and 5n exhibited higher levels of efficacy than fluoxetine in the forced swimming test.
• Compound 5i exhibited greater efficacy than fluoxetine in the tail suspension test.
• Compounds 5c and 5d showed moderate levels of anticonvulsant activity in the maximal electroshock seizure screen.

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 5i 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.

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.Figure optionsDownload as PowerPoint slide