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Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates

The development of novel antimicrobial agents represents a timely research topic. Eighteen salicylanilide 4-(trifluoromethyl)benzoates were evaluated against Mycobacterium tuberculosis, M. avium and M. kansasii, eight bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA) and...

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Autores principales: Krátký, Martin, Vinšová, Jarmila, Novotná, Eva, Mandíková, Jana, Trejtnar, František, Stolaříková, Jiřina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270420/
https://www.ncbi.nlm.nih.gov/pubmed/23529028
http://dx.doi.org/10.3390/molecules18043674
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author Krátký, Martin
Vinšová, Jarmila
Novotná, Eva
Mandíková, Jana
Trejtnar, František
Stolaříková, Jiřina
author_facet Krátký, Martin
Vinšová, Jarmila
Novotná, Eva
Mandíková, Jana
Trejtnar, František
Stolaříková, Jiřina
author_sort Krátký, Martin
collection PubMed
description The development of novel antimicrobial agents represents a timely research topic. Eighteen salicylanilide 4-(trifluoromethyl)benzoates were evaluated against Mycobacterium tuberculosis, M. avium and M. kansasii, eight bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA) and for the inhibition of mycobacterial isocitrate lyase. Some compounds were further screened against drug-resistant M. tuberculosis and for their cytotoxicity. Minimum inhibitory concentrations (MICs) for all mycobacterial strains were within 0.5–32 μmol/L, with 4-chloro-2-[4-(trifluoromethyl)phenylcarbamoyl]phenyl 4-(trifluoromethyl)benzoate superiority. Gram-positive bacteria including MRSA were inhibited with MICs ≥ 0.49 μmol/L, while Gram-negative ones were much less susceptible. Salicylanilide 4-(trifluoromethyl)benzoates showed significant antibacterial properties, for many strains being comparable to standard drugs (isoniazid, benzylpenicillin) with no cross-resistance. All esters showed mild inhibition of mycobacterial isocitrate lyase and four compounds were comparable to 3-nitropropionic acid without a direct correlation between in vitro MICs and enzyme inhibition.
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spelling pubmed-62704202018-12-14 Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates Krátký, Martin Vinšová, Jarmila Novotná, Eva Mandíková, Jana Trejtnar, František Stolaříková, Jiřina Molecules Article The development of novel antimicrobial agents represents a timely research topic. Eighteen salicylanilide 4-(trifluoromethyl)benzoates were evaluated against Mycobacterium tuberculosis, M. avium and M. kansasii, eight bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA) and for the inhibition of mycobacterial isocitrate lyase. Some compounds were further screened against drug-resistant M. tuberculosis and for their cytotoxicity. Minimum inhibitory concentrations (MICs) for all mycobacterial strains were within 0.5–32 μmol/L, with 4-chloro-2-[4-(trifluoromethyl)phenylcarbamoyl]phenyl 4-(trifluoromethyl)benzoate superiority. Gram-positive bacteria including MRSA were inhibited with MICs ≥ 0.49 μmol/L, while Gram-negative ones were much less susceptible. Salicylanilide 4-(trifluoromethyl)benzoates showed significant antibacterial properties, for many strains being comparable to standard drugs (isoniazid, benzylpenicillin) with no cross-resistance. All esters showed mild inhibition of mycobacterial isocitrate lyase and four compounds were comparable to 3-nitropropionic acid without a direct correlation between in vitro MICs and enzyme inhibition. MDPI 2013-03-25 /pmc/articles/PMC6270420/ /pubmed/23529028 http://dx.doi.org/10.3390/molecules18043674 Text en © 2013 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
Novotná, Eva
Mandíková, Jana
Trejtnar, František
Stolaříková, Jiřina
Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates
title Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates
title_full Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates
title_fullStr Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates
title_full_unstemmed Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates
title_short Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates
title_sort antibacterial activity of salicylanilide 4-(trifluoromethyl)benzoates
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270420/
https://www.ncbi.nlm.nih.gov/pubmed/23529028
http://dx.doi.org/10.3390/molecules18043674
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