title: Antimycobacterial assessment of Salicylanilide benzoates including multidrug-resistant tuberculosis strains.
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 &#956;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&#8211;2 &#956;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&#8211;1 &#956;mol/L). Unfortunately, the most potent esters were still considerably cytotoxic, although mostly less than their parent salicylanilides.
authors.affiliation: Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, Hradec Králové 50005, Czech Republic. martin.kratky@faf.cuni.cz
authors.forename: Martin
authors.initials: M
authors.lastname: Krátký
authors.forename: Jarmila
authors.initials: J
authors.lastname: Vinšová
authors.forename: Jiřina
authors.initials: J
authors.lastname: Stolaříková
mesh_terms: D000995:Antitubercular Agents / Q000494:pharmacology* / Q000633:toxicity; D001565:Benzoates / Q000494:pharmacology* / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D024901:Drug Resistance, Multiple, Bacterial; D056945:Hep G2 Cells; D006801:Humans; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D009162:Mycobacterium avium / Q000187:drug effects; D019909:Mycobacterium kansasii / Q000187:drug effects; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D012458:Salicylanilides / Q000494:pharmacology* / Q000633:toxicity
chemical_list: D000995:Antitubercular Agents; D001565:Benzoates; D012458:Salicylanilides