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

Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains

1
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1,*  and 2
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.
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
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.

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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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