Molecules 2012, 17(11), 12812-12820; doi:10.3390/molecules171112812
Article

Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains

1 Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, Hradec Králové 50005, Czech Republic 2 Laboratory for Mycobacterial Diagnostics and Tuberculosis, Regional Institute of Public Health in Ostrava, Partyzánské náměstí 7, Ostrava 70200, Czech Republic
* Author to whom correspondence should be addressed.
Received: 19 September 2012; in revised form: 24 October 2012 / Accepted: 26 October 2012 / Published: 31 October 2012
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Abstract: 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.
Keywords: antimycobacterial activity; benzoic acid ester; cytotoxicity; in vitro activity; multidrug-resistant tuberculosis; salicylanilide; salicylanilide ester

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MDPI and ACS Style

Krátký, M.; Vinšová, J.; Stolaříková, J. Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains. Molecules 2012, 17, 12812-12820.

AMA Style

Krátký M, Vinšová J, Stolaříková J. Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains. Molecules. 2012; 17(11):12812-12820.

Chicago/Turabian Style

Krátký, Martin; Vinšová, Jarmila; Stolaříková, Jiřina. 2012. "Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains." Molecules 17, no. 11: 12812-12820.

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