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

Thirty-four new benzo[d]thiazol derivatives 2a–2i, 3a–3r, and 4a–4g 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 percent...

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Detalles Bibliográficos
Autores principales: Jin, Qinghao, Fu, Zhiyang, Guan, Liping, Jiang, Haiying
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6669756/
https://www.ncbi.nlm.nih.gov/pubmed/31340514
http://dx.doi.org/10.3390/md17070430
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author Jin, Qinghao
Fu, Zhiyang
Guan, Liping
Jiang, Haiying
author_facet Jin, Qinghao
Fu, Zhiyang
Guan, Liping
Jiang, Haiying
author_sort Jin, Qinghao
collection PubMed
description Thirty-four new benzo[d]thiazol derivatives 2a–2i, 3a–3r, and 4a–4g 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 ED(50) values of 46.1 and 64.3 mg kg(−)(1), 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.
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spelling pubmed-66697562019-08-08 Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects Jin, Qinghao Fu, Zhiyang Guan, Liping Jiang, Haiying Mar Drugs Article Thirty-four new benzo[d]thiazol derivatives 2a–2i, 3a–3r, and 4a–4g 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 ED(50) values of 46.1 and 64.3 mg kg(−)(1), 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. MDPI 2019-07-23 /pmc/articles/PMC6669756/ /pubmed/31340514 http://dx.doi.org/10.3390/md17070430 Text en © 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Jin, Qinghao
Fu, Zhiyang
Guan, Liping
Jiang, Haiying
Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects
title Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects
title_full Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects
title_fullStr Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects
title_full_unstemmed Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects
title_short Syntheses of Benzo[d]Thiazol-2(3H)-One Derivatives and Their Antidepressant and Anticonvulsant Effects
title_sort syntheses of benzo[d]thiazol-2(3h)-one derivatives and their antidepressant and anticonvulsant effects
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6669756/
https://www.ncbi.nlm.nih.gov/pubmed/31340514
http://dx.doi.org/10.3390/md17070430
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