Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67179843%3A_____%2F15%3A00446420" target="_blank" >RIV/67179843:_____/15:00446420 - isvavai.cz</a>
Alternative codes found
RIV/62157124:16370/15:43873805
Result on the web
<a href="http://dx.doi.org/10.1016/j.bmc.2015.06.047" target="_blank" >http://dx.doi.org/10.1016/j.bmc.2015.06.047</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmc.2015.06.047" target="_blank" >10.1016/j.bmc.2015.06.047</a>

Result language
angličtina
Original language name
Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents
Original language description
In this study, a series of twenty-two ring-substituted 8-hydroxyquinoline-2-carboxanilides was prepared and characterized. Primary in vitro screening of the synthesized compounds was performed against Mycobacterium tuberculosis H37Ra, Mycobacterium avium complex and M. avium subsp. paratuberculosis. Some of the tested compounds showed the antimycobacterial activity against M. avium subsp. paratuberculosis comparable with or higher than that of rifampicin. 8-Hydroxy-N-[3-(trifluoromethyl)phenyl]- and 8-hydroxy-N-[4-(trifluoromethyl)phenyl]quinoline-2-carboxamide showed MIC=24μM against all tested mycobacterial strains. 3-Methoxyphenyl- and 3-methylphenyl derivatives expressed MIC=27 or 29μM also against all the tested strains. Their activity against M. avium subsp. paratuberculosis was 4-fold higher than that of rifampicin. 2-Bromophenyl- and 2-(trifluoromethyl)phenyl derivatives had MIC=23 or 24μM against M. tuberculosis. A significant decrease of mycobacterial cell metabolism (viability of M. tuberculosis H37Ra) was observed using MTT assay. Screening of cytotoxicity of the compounds was performed using the THP-1 cells, and no significant lethal effect was observed up to tested concentration 30μM. The structure-activity relationships are discussed.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
CE - Biochemistry
OECD FORD branch
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Project
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Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2015
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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