Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62157124%3A16370%2F15%3A43873818" target="_blank" >RIV/62157124:16370/15:43873818 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1016/j.bmc.2015.03.018" target="_blank" >http://dx.doi.org/10.1016/j.bmc.2015.03.018</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.bmc.2015.03.018" target="_blank" >10.1016/j.bmc.2015.03.018</a>

Result language
angličtina
Original language name
Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides
Original language description
In this study, a series of twenty-two ring-substituted 6-hydroxynaphthalene-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. Derivatives substituted by trifluoromethyl, bromo, methyl and methoxy moieties in C-(3)' and C-(4)' positions of the anilide ring showed 2-fold higher activity against M. tuberculosis than isoniazid and 4.5-fold higher activity against M. avium subsp. paratuberculosis than rifampicin. 6-Hydroxy-N-(2-methylphenyl) naphthalene-2-carboxamide had MIC = 29 mu M against M. avium complex. A significant decrease of mycobacterial cell metabolism (viability of M. tuberculosis H37Ra) was observed using MTT assay. Screening of the cytotoxicity of the most effective antimycobacterial compounds was performed using the THP-1 cells, and no significant lethal effect was observed. The structure-activity relationships are discussed.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30104 - Pharmacology and pharmacy

Project
<a href="/en/project/EE2.3.30.0053" target="_blank" >EE2.3.30.0053: Pharmaco-toxicological evaluation of newly synthesized (isolated) compounds as an integration tool for pre-clinical disciplines at VFU Brno</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach

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

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