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Open AccessArticle

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

1
Donghai Science and Technology College, Zhejiang Ocean University, Zhoushan 316000, China
2
Food and Pharmacy College, Zhejiang Ocean University, Zhoushan 316022, China
3
College of Medicine, Jiaxing University, Jiaxing 314001, China
*
Authors to whom correspondence should be addressed.
Mar. Drugs 2019, 17(7), 430; https://doi.org/10.3390/md17070430
Received: 4 July 2019 / Revised: 18 July 2019 / Accepted: 19 July 2019 / Published: 23 July 2019
(This article belongs to the Special Issue Synthetic and Biosynthetic Approaches to Marine Natural Products)
Thirty-four new benzo[d]thiazol derivatives 2a2i, 3a3r, and 4a4g were synthesized and investigated for their potential antidepressant and anticonvulsant effects. In a forced swimming test, 2c and 2d showed the highest antidepressant and anticonvulsant effects. 2c and 2d 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, 3n and 3q showed the highest anticonvulsant effect, with ED50 values of 46.1 and 64.3 mg kg1, 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 2c and 2d may be via increasing the concentrations of serotonin and norepinephrine. View Full-Text
Keywords: benzo[d]thiazol; synthesis; antarctic-derived fungus; antidepressant; anticonvulsant benzo[d]thiazol; synthesis; antarctic-derived fungus; antidepressant; anticonvulsant
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MDPI and ACS Style

Jin, Q.; Fu, Z.; Guan, L.; Jiang, H. Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects. Mar. Drugs 2019, 17, 430.

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