Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates

Molecules

Martin Krátký¹  Jarmila Vinšová¹  Eva Novotná³  Jana Mandíková²  Frantiᘞk Trejtnar² 

[1] Department of Inorganic and Organic Chemistry, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic; E-Mail:;Department of Pharmacology and Toxicology, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic; E-Mails:;Department of Biochemical Sciences, Faculty of Pharmacy, Charles University, Heyrovského 1203, 500 05 Hradec Králové, Czech Republic; E-Mail:

关键词: antibacterial activity;    antimycobacterial activity;    cytotoxicity;    isocitrate lyase inhibitor;    multidrug-resistant tuberculosis;    salicylanilide ester;    4-(trifluoromethyl)benzoic acid ester;   

DOI  :  10.3390/molecules18043674

来源: mdpi

【 摘 要 】

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 μmol/L, with 4-chloro-2-[4-(trifluoromethyl)phenylcarbamoyl]phenyl 4-(trifluoromethyl)benzoate superiority. Gram-positive bacteria including MRSA were inhibited with MICs ≥ 0.49 μmol/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.

【 授权许可】

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© 2013 by the authors; licensee MDPI, Basel, Switzerland.