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Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains
The increasing emergence especially of drug-resistant tuberculosis has led to a strong demand for new anti-tuberculosis drugs. Eighteen salicylanilide benzoates were evaluated for their inhibition potential against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kans...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2012
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268668/ https://www.ncbi.nlm.nih.gov/pubmed/23114617 http://dx.doi.org/10.3390/molecules171112812 |
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author | Krátký, Martin Vinšová, Jarmila Stolaříková, Jiřina |
author_facet | Krátký, Martin Vinšová, Jarmila Stolaříková, Jiřina |
author_sort | Krátký, Martin |
collection | PubMed |
description | The increasing emergence especially of drug-resistant tuberculosis has led to a strong demand for new anti-tuberculosis drugs. Eighteen salicylanilide benzoates were evaluated for their inhibition potential against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii; minimum inhibitory concentration values ranged from 0.5 to 16 μmol/L. The most active esters underwent additional biological assays. Four benzoates inhibited effectively the growth of five multidrug-resistant strains and one extensively drug-resistant strain of M. tuberculosis at low concentrations (0.25–2 μmol/L) regardless of the resistance patterns. The highest rate of multidrug-resistant mycobacteria inhibition expressed 4-chloro-2-[4-(trifluoromethyl)-phenylcarbamoyl]phenyl benzoate (0.25–1 μmol/L). Unfortunately, the most potent esters were still considerably cytotoxic, although mostly less than their parent salicylanilides. |
format | Online Article Text |
id | pubmed-6268668 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2012 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62686682018-12-13 Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains Krátký, Martin Vinšová, Jarmila Stolaříková, Jiřina Molecules Article The increasing emergence especially of drug-resistant tuberculosis has led to a strong demand for new anti-tuberculosis drugs. Eighteen salicylanilide benzoates were evaluated for their inhibition potential against Mycobacterium tuberculosis, Mycobacterium avium and two strains of Mycobacterium kansasii; minimum inhibitory concentration values ranged from 0.5 to 16 μmol/L. The most active esters underwent additional biological assays. Four benzoates inhibited effectively the growth of five multidrug-resistant strains and one extensively drug-resistant strain of M. tuberculosis at low concentrations (0.25–2 μmol/L) regardless of the resistance patterns. The highest rate of multidrug-resistant mycobacteria inhibition expressed 4-chloro-2-[4-(trifluoromethyl)-phenylcarbamoyl]phenyl benzoate (0.25–1 μmol/L). Unfortunately, the most potent esters were still considerably cytotoxic, although mostly less than their parent salicylanilides. MDPI 2012-10-31 /pmc/articles/PMC6268668/ /pubmed/23114617 http://dx.doi.org/10.3390/molecules171112812 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Krátký, Martin Vinšová, Jarmila Stolaříková, Jiřina Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains |
title | Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains |
title_full | Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains |
title_fullStr | Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains |
title_full_unstemmed | Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains |
title_short | Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains |
title_sort | antimycobacterial assessment of salicylanilide benzoates including multidrug-resistant tuberculosis strains |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268668/ https://www.ncbi.nlm.nih.gov/pubmed/23114617 http://dx.doi.org/10.3390/molecules171112812 |
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