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.
Highlights
Tuberculosis (TB) represents a contagious infectious disease caused by Mycobacterium tuberculosis complex
The synthesis and characterization (m.p., IR and NMR spectra, elemental analyses) of salicylanilide benzoates [2-(phenylcarbamoyl)phenyl benzoates; 1] were published recently [17]; their synthetic route is depicted in Scheme 1
The masking of salicylanilide phenolic group by lipophilic aromatic acid resulted in the derivatives with improved antimycobacterial potency in the micromolar range (0.25–16 μmol/L)
Summary
Tuberculosis (TB) represents a contagious infectious disease caused by Mycobacterium tuberculosis complex. Salicylanilide (2-hydroxy-N-phenylbenzamide) derivatives may be such a promising group with a complex mechanism of action [7] Their various esters have exhibited a significant antimycobacterial activity in micromolar or lower concentrations, including MDR-TB and atypical mycobacteria; they do not share any resistance with established antimycobacterial drugs. This study brings a complex characteristic of antimycobacterial properties (including against atypical, MDR- and XDR-TB strains) of known salicylanilide benzoates. It is a part of our research effort concerned with a group of salicylanilide derivatives with improved activity and/or reduced toxicity in comparison to their parent molecules
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