Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates

作者：Kratky Martin; Vinsova Jarmila^*; Novotna Eva; Mandikova Jana; Trejtnar Frantisek; Stolarikova Jirina

来源：Molecules, 2013, 18(4): 3674-3688.

DOI：10.3390/molecules18043674

• antibacterial activity
• antimycobacterial activity
• cytotoxicity
• isocitrate lyase inhibitor
• multidrug-resistant tuberculosis
• salicylanilide ester
• 4-(trifluoromethyl)benzoic acid ester

The development of novel antimicrobial agents represents a timely research topic. Eighteen salicylanilide 4-(trifluoromethyl)benzoates were evaluated against Mycobacterium tuberculosis, M. avium and M. kansasii, eight bacterial strains including methicillin-resistant Staphylococcus aureus (MRSA) and for the inhibition of mycobacterial isocitrate lyase. Some compounds were further screened against drug-resistant M. tuberculosis and for their cytotoxicity. Minimum inhibitory concentrations (MICs) for all mycobacterial strains were within 0.5-32 mu mol/L, with 4-chloro-2-[4-(trifluoromethyl)phenylcarbamoyl] phenyl 4-(trifluoromethyl) benzoate superiority. Grampositive bacteria including MRSA were inhibited with MICs %26gt;= 0.49 mu mol/L, while Gram-negative ones were much less susceptible. Salicylanilide 4-(trifluoromethyl) benzoates showed significant antibacterial properties, for many strains being comparable to standard drugs (isoniazid, benzylpenicillin) with no cross-resistance. All esters showed mild inhibition of mycobacterial isocitrate lyase and four compounds were comparable to 3-nitropropionic acid without a direct correlation between in vitro MICs and enzyme inhibition.

• 出版日期2013-4