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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...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2019
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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. |
format | Online Article Text |
id | pubmed-6669756 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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