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