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Molecules 2013, 18(4), 3674-3688; doi:10.3390/molecules18043674
Article

Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)-benzoates

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1,* , 2
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1 Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic 2 Department of Biochemical Sciences, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic 3 Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic 4 Laboratory for Mycobacterial Diagnostics and Tuberculosis, Regional Institute of Public Health in Ostrava, Partyzánské náměstí 7, 702 00 Ostrava, Czech Republic
* Author to whom correspondence should be addressed.
Received: 1 February 2013 / Revised: 18 March 2013 / Accepted: 18 March 2013 / Published: 25 March 2013
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Abstract

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 ³ 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.
Keywords: antibacterial activity; antimycobacterial activity; cytotoxicity; isocitrate lyase inhibitor; multidrug-resistant tuberculosis; salicylanilide ester; 4-(trifluoromethyl)benzoic acid ester antibacterial activity; antimycobacterial activity; cytotoxicity; isocitrate lyase inhibitor; multidrug-resistant tuberculosis; salicylanilide ester; 4-(trifluoromethyl)benzoic acid ester
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Krátký, M.; Vinšová, J.; Novotná, E.; Mandíková, J.; Trejtnar, F.; Stolaříková, J. Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)-benzoates. Molecules 2013, 18, 3674-3688.

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