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苯并噻唑-2(3H)-酮衍生物的合成及其抗抑郁和抗惊厥作用。

Syntheses of Benzo[]Thiazol-2(3)-One Derivatives and Their Antidepressant and Anticonvulsant Effects.

机构信息

Donghai Science and Technology College, Zhejiang Ocean University, Zhoushan 316000, China.

Food and Pharmacy College, Zhejiang Ocean University, Zhoushan 316022, China.

出版信息

Mar Drugs. 2019 Jul 23;17(7):430. doi: 10.3390/md17070430.

Abstract

Thirty-four new benzo[]thiazol derivatives -, -, and - were synthesized and investigated for their potential antidepressant and anticonvulsant effects. In a forced swimming test, and showed the highest antidepressant and anticonvulsant effects. and displayed a higher percentage decrease in immobility duration (89.96% and 89.62%, respectively) than that of fluoxetine (83.62%). In the maximal electroshock seizure test, and showed the highest anticonvulsant effect, with ED values of 46.1 and 64.3 mg kg, and protective indices of 6.34 and 4.11, respectively, which were similar to those of phenobarbital or valproate. We also found that the mechanism for the antidepressant activity of and may be via increasing the concentrations of serotonin and norepinephrine.

摘要

合成了 34 种新的苯并噻唑衍生物 - 、 - 和 - ,并研究了它们潜在的抗抑郁和抗惊厥作用。在强迫游泳试验中, 和 表现出最高的抗抑郁和抗惊厥作用。 和 显示出更高的不动时间百分比降低(分别为 89.96%和 89.62%),高于氟西汀(83.62%)。在最大电休克惊厥试验中, 和 表现出最高的抗惊厥作用,ED 值分别为 46.1 和 64.3 mg kg,保护指数分别为 6.34 和 4.11,与苯巴比妥或丙戊酸相似。我们还发现, 和 抗抑郁作用的机制可能是通过增加 5-羟色胺和去甲肾上腺素的浓度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1e7a/6669756/949198aa36c5/marinedrugs-17-00430-g001.jpg

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