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A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate
A long list of chemotherapeutical drugs used in the treatment of the peripheral and the central nervous systems possess anti-microbial activity. Some of these neurotropic compounds are chiral, with the one stereo isomeric form exaggerating reduced neurotropism. This is the case for the levorotatory...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Public Library of Science
2013
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3591432/ https://www.ncbi.nlm.nih.gov/pubmed/23505431 http://dx.doi.org/10.1371/journal.pone.0057493 |
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author | Christensen, Jørn B. Hendricks, Oliver Chaki, Shaswati Mukherjee, Sayanti Das, Ayan Pal, Tapan K. Dastidar, Sujata G. Kristiansen, Jette E. |
author_facet | Christensen, Jørn B. Hendricks, Oliver Chaki, Shaswati Mukherjee, Sayanti Das, Ayan Pal, Tapan K. Dastidar, Sujata G. Kristiansen, Jette E. |
author_sort | Christensen, Jørn B. |
collection | PubMed |
description | A long list of chemotherapeutical drugs used in the treatment of the peripheral and the central nervous systems possess anti-microbial activity. Some of these neurotropic compounds are chiral, with the one stereo isomeric form exaggerating reduced neurotropism. This is the case for the levorotatory form of thioridazine. The phenothiazine thioridazine is an interesting compound, characterized by exhibiting a significant growth inhibiting activity on a wide array of micro-organisms. Thioridazine is characterized by another challenging feature, because the compound is concentrated in certain human tissue cells. The present study describes a comparative study of the two enantiomers as well as the racemic form of thioridazine. The study exploits the stereochemical aspect and the in vitro and in vivo potential of these compounds, with a focus on the effects on Gram negative organism Salmonella enterica serover Typhimurium. In summary, the results of this study yielded a significant antibacterial activity of all forms of thioridazine, indicating the levorotatory (–)- form to be superior in terms of both its in vitro and in vivo efficacies. |
format | Online Article Text |
id | pubmed-3591432 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2013 |
publisher | Public Library of Science |
record_format | MEDLINE/PubMed |
spelling | pubmed-35914322013-03-15 A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate Christensen, Jørn B. Hendricks, Oliver Chaki, Shaswati Mukherjee, Sayanti Das, Ayan Pal, Tapan K. Dastidar, Sujata G. Kristiansen, Jette E. PLoS One Research Article A long list of chemotherapeutical drugs used in the treatment of the peripheral and the central nervous systems possess anti-microbial activity. Some of these neurotropic compounds are chiral, with the one stereo isomeric form exaggerating reduced neurotropism. This is the case for the levorotatory form of thioridazine. The phenothiazine thioridazine is an interesting compound, characterized by exhibiting a significant growth inhibiting activity on a wide array of micro-organisms. Thioridazine is characterized by another challenging feature, because the compound is concentrated in certain human tissue cells. The present study describes a comparative study of the two enantiomers as well as the racemic form of thioridazine. The study exploits the stereochemical aspect and the in vitro and in vivo potential of these compounds, with a focus on the effects on Gram negative organism Salmonella enterica serover Typhimurium. In summary, the results of this study yielded a significant antibacterial activity of all forms of thioridazine, indicating the levorotatory (–)- form to be superior in terms of both its in vitro and in vivo efficacies. Public Library of Science 2013-03-07 /pmc/articles/PMC3591432/ /pubmed/23505431 http://dx.doi.org/10.1371/journal.pone.0057493 Text en © 2013 Christensen et al http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are properly credited. |
spellingShingle | Research Article Christensen, Jørn B. Hendricks, Oliver Chaki, Shaswati Mukherjee, Sayanti Das, Ayan Pal, Tapan K. Dastidar, Sujata G. Kristiansen, Jette E. A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate |
title | A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate |
title_full | A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate |
title_fullStr | A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate |
title_full_unstemmed | A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate |
title_short | A comparative Analysis of In Vitro and In Vivo Efficacies of the Enantiomers of Thioridazine and Its Racemate |
title_sort | comparative analysis of in vitro and in vivo efficacies of the enantiomers of thioridazine and its racemate |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3591432/ https://www.ncbi.nlm.nih.gov/pubmed/23505431 http://dx.doi.org/10.1371/journal.pone.0057493 |
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