Letters in Drug Design & Discovery

Author(s): Yu Sun, Qing-Hao Jin, Yan Han, Di Yu, Qiu-Ping Dai and Zhou-Jun Zheng

DOI: 10.2174/1570180813666160826113018

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Design, Synthesis and Antidepressant and Anticonvulsant Effect of 1-Alkoxy-1H-Benzo[d]-1,2,3-Triazole Derivatives

Page: [314 - 322] Pages: 9

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Abstract

Background: 21 novel 1-alkoxy-1H-benzo[d]-1,2,3-triazole compounds were designed, prepared and evaluated for their antidepressant and anticonvulsant effects in mice.

Method: Compound 19 significantly decreased immobility time in the FST without altering the locomotor activity in the open field test, and exhibited higher levels of efficacy than the reference standard fluoxetine. Compound 19 significantly increased 5-HT, NE and 5-HIAA levels in mice brain, implying that the antidepressant activity might be mediated by these neurotransmitters. In the seizure test, compound 19 also showed better anticonvulsant activity against MES, whereas had not shown neurotoxicity (300 mg/kg).

Conclusion: Our data indicated that compound 19 could potentially be used as the antidepressant drug in patients with epilepsy.

Keywords: Benzo[d]-1, 2, 3-triazole, FST, neurotransmitters, MES, antidepressant.