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

Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)-benzoates

Received: 1 February 2013; in revised form: 18 March 2013 / Accepted: 18 March 2013 / Published: 25 March 2013
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
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
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MDPI and ACS Style

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

AMA Style

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

Chicago/Turabian Style

Krátký, Martin; Vinšová, Jarmila; Novotná, Eva; Mandíková, Jana; Trejtnar, František; Stolaříková, Jiřina. 2013. "Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)-benzoates." Molecules 18, no. 4: 3674-3688.

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