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@article{1409330,
author = {Kos, J and Nevin, E and Soral, M and Kushkevych, Ivan and Goněc, Tomáš and Bobáľ, Pavel and Kollár, Peter and Coffey, A and J, O Mahony and Liptaj, T and Kralova, K and Jampilek, J},
article_location = {OXFORD},
article_number = {9},
doi = {http://dx.doi.org/10.1016/j.bmc.2015.03.018},
keywords = {Hydroxynaphthalene-2-carboxanilides; In vitro antimycobacterial activity; MTT assay; In vitro cytotoxicity; Structure-activity relationships},
language = {eng},
issn = {0968-0896},
journal = {BIOORGANIC & MEDICINAL CHEMISTRY},
note = {Doc. Kushkevychovi chybí na WoS afiliace na MU, nelze přenášet do RIV!},
title = {Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides},
url = {http://dx.doi.org/10.1016/j.bmc.2015.03.018},
volume = {23},
year = {2015}
}
TY - JOUR
ID - 1409330
AU - Kos, J - Nevin, E - Soral, M - Kushkevych, Ivan - Goněc, Tomáš - Bobáľ, Pavel - Kollár, Peter - Coffey, A - J, O Mahony - Liptaj, T - Kralova, K - Jampilek, J
PY - 2015
TI - Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides
JF - BIOORGANIC & MEDICINAL CHEMISTRY
VL - 23
IS - 9
SP - 2035-2043
EP - 2035-2043
PB - PERGAMON-ELSEVIER SCIENCE LTD
SN - 09680896
N1 - Doc. Kushkevychovi chybí na WoS afiliace na MU, nelze přenášet do RIV!
KW - Hydroxynaphthalene-2-carboxanilides
KW - In vitro antimycobacterial activity
KW - MTT assay
KW - In vitro cytotoxicity
KW - Structure-activity relationships
UR - http://dx.doi.org/10.1016/j.bmc.2015.03.018
L2 - http://dx.doi.org/10.1016/j.bmc.2015.03.018
N2 - 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. (C) 2015 Elsevier Ltd. All rights reserved.
ER -
KOS, J, E NEVIN, M SORAL, Ivan KUSHKEVYCH, Tomáš GONĚC, Pavel BOBÁĽ, Peter KOLLÁR, A COFFEY, O Mahony J, T LIPTAJ, K KRALOVA a J JAMPILEK. Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides. \textit{BIOORGANIC \&{}amp; MEDICINAL CHEMISTRY}. OXFORD: PERGAMON-ELSEVIER SCIENCE LTD, 2015, roč.~23, č.~9, s.~2035-2043. ISSN~0968-0896. Dostupné z: https://dx.doi.org/10.1016/j.bmc.2015.03.018.
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