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- Title
Antibacterial Activity of Salicylanilide 4-(Trifluoromethyl)benzoates.
- Authors
Krátký, Martin; VinŠová, Jarmila; Novotná, Eva; Mandíková, Jana; Trejtnar, FrantiŠek; Stolaříková, Jiřina
- Abstract
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. Grampositive bacteria including MRSA were inhibited with MICs ⩾ 0.49 μmol/L, while Gramnegative 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.
- Subjects
SALICYLANILIDES; TRIFLUOROMETHYL compounds; BENZOATES; ANTIBACTERIAL agents; MYCOBACTERIUM tuberculosis; ISONIAZID; PENICILLIN G
- Publication
Molecules, 2013, Vol 18, Issue 4, p3674
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules18043674