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

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 / Revised: 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. View Full-Text
Keywords: antimycobacterial activity; benzoic acid ester; cytotoxicity; in vitro activity; multidrug-resistant tuberculosis; salicylanilide; salicylanilide ester antimycobacterial activity; benzoic acid ester; cytotoxicity; in vitro activity; multidrug-resistant tuberculosis; salicylanilide; salicylanilide ester
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Krátký, M.; Vinšová, J.; Stolaříková, J. Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains. Molecules 2012, 17, 12812-12820.

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