| KOS, J, I ZADRAZILOVA, E NEVIN, M SORAL, Tomáš GONĚC, Peter KOLLÁR, M ORAVEC, A COFFEY, O Mahony J, T LIPTAJ, K KRALOVA a J JAMPILEK. Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents. Online. BIOORGANIC & MEDICINAL CHEMISTRY. OXFORD: PERGAMON-ELSEVIER SCIENCE LTD, 2015, roč. 23, č. 15, s. 4188-4196. ISSN 0968-0896. Dostupné z: https://dx.doi.org/10.1016/j.bmc.2015.06.047. [citováno 2024-04-23] |
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@article{1727163,
author = {Kos, J and Zadrazilova, I and Nevin, E and Soral, M and Goněc, Tomáš and Kollár, Peter and Oravec, M and Coffey, A and J, O Mahony and Liptaj, T and Kralova, K and Jampilek, J},
article_location = {OXFORD},
article_number = {15},
doi = {http://dx.doi.org/10.1016/j.bmc.2015.06.047},
keywords = {8-Hydroxyquinolines; In vitro antimycobacterial activity; MTT assay; In vitro cytotoxicity; Structure-activity relationships},
language = {eng},
issn = {0968-0896},
journal = {BIOORGANIC & MEDICINAL CHEMISTRY},
title = {Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents},
volume = {23},
year = {2015}
}
TY - JOUR
ID - 1727163
AU - Kos, J - Zadrazilova, I - Nevin, E - Soral, M - Goněc, Tomáš - Kollár, Peter - Oravec, M - Coffey, A - J, O Mahony - Liptaj, T - Kralova, K - Jampilek, J
PY - 2015
TI - Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents
JF - BIOORGANIC & MEDICINAL CHEMISTRY
VL - 23
IS - 15
SP - 4188-4196
EP - 4188-4196
PB - PERGAMON-ELSEVIER SCIENCE LTD
SN - 09680896
KW - 8-Hydroxyquinolines
KW - In vitro antimycobacterial activity
KW - MTT assay
KW - In vitro cytotoxicity
KW - Structure-activity relationships
N2 - 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 = 24 mu M against all tested mycobacterial strains. 3-Methoxyphenyl- and 3-methylphenyl derivatives expressed MIC = 27 or 29 mu M 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 24 mu M 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 30 mu M. The structure-activity relationships are discussed. (C) 2015 Elsevier Ltd. All rights reserved.
ER -
KOS, J, I ZADRAZILOVA, E NEVIN, M SORAL, Tomáš GONĚC, Peter KOLLÁR, M ORAVEC, A COFFEY, O Mahony J, T LIPTAJ, K KRALOVA a J JAMPILEK. Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents. Online. \textit{BIOORGANIC \&{}amp; MEDICINAL CHEMISTRY}. OXFORD: PERGAMON-ELSEVIER SCIENCE LTD, 2015, roč.~23, č.~15, s.~4188-4196. ISSN~0968-0896. Dostupné z: https://dx.doi.org/10.1016/j.bmc.2015.06.047. [citováno 2024-04-23]
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