Design, Synthesis and Antidepressant and Anticonvulsant Effect of 1-Alkoxy-1H-Benzo[d]-1,2,3-Triazole Derivatives
作者:Yu Sun、Qing-Hao Jin、Yan Han、Di Yu、Qiu-Ping Dai、Zhou-Jun Zheng
DOI:10.2174/1570180813666160826113018
日期:2017.1.26
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.
背景:设计、制备并评估了21种新型1-烷氧基-1H-苯并[d]-1,2,3-噻唑化合物在小鼠中的抗抑郁和抗惊厥效果。
方法:化合物19在强迫游泳试验(FST)中显著减少了动物的失动时间,而不改变开放场实验中的运动活动,其疗效高于参照标准药物氟西汀。化合物19显著提高了小鼠大脑中5-HT、NE和5-HIAA的水平,这表明其抗抑郁活性可能与这些神经递质有关。在癫痫测试中,化合物19在对抗MES方面也表现出更好的抗惊厥活性,同时没有显示出神经毒性(300 mg/kg)。
结论:我们的数据表明,化合物19可能作为抗抑郁药用于癫痫患者。