Antimycobacterial Assessment of Salicylanilide Benzoates including Multidrug-Resistant Tuberculosis Strains

作者：Kratky Martin; Vinsova Jarmila^*; Stolarikova Jirina

来源：Molecules, 2012, 17(11): 12812-12820.

DOI：10.3390/molecules171112812

• antimycobacterial activity
• benzoic acid ester
• cytotoxicity
• in vitro activity
• multidrug-resistant tuberculosis
• salicylanilide
• salicylanilide ester

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 mu mol/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 mu mol/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 mu mol/L). Unfortunately, the most potent esters were still considerably cytotoxic, although mostly less than their parent salicylanilides.

• 出版日期2012-11