| GONĚC, Tomáš, S POSPISILOVA, L HOLANOVA, J STRANIK, A CERNIKOVA, V PUDELKOVA, J KOS, M ORAVEC, Peter KOLLÁR, Alois ČÍŽEK a J JAMPILEK. Synthesis and Antimicrobial Evaluation of 1-[(2-Substituted phenyl)carbamoyl]naphthalen-2-yl Carbamates. Molecules. BASEL: Mayer und Muller, 2016, roč. 21, č. 9, 15 s. ISSN 1420-3049. Dostupné z: https://dx.doi.org/10.3390/molecules21091189. |
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@article{1727184,
author = {Goněc, Tomáš and Pospisilova, S and Holanova, L and Stranik, J and Cernikova, A and Pudelkova, V and Kos, J and Oravec, M and Kollár, Peter and Čížek, Alois and Jampilek, J},
article_location = {BASEL},
article_number = {9},
doi = {http://dx.doi.org/10.3390/molecules21091189},
keywords = {carbamates; hydroxynaphthalene-carboxamides; in vitro antibacterial activity; in vitro antimycobacterial activity; in vitro cytotoxicity assay; structure-activity relationships},
language = {eng},
issn = {1420-3049},
journal = {Molecules},
title = {Synthesis and Antimicrobial Evaluation of 1-[(2-Substituted phenyl)carbamoyl]naphthalen-2-yl Carbamates},
volume = {21},
year = {2016}
}
TY - JOUR
ID - 1727184
AU - Goněc, Tomáš - Pospisilova, S - Holanova, L - Stranik, J - Cernikova, A - Pudelkova, V - Kos, J - Oravec, M - Kollár, Peter - Čížek, Alois - Jampilek, J
PY - 2016
TI - Synthesis and Antimicrobial Evaluation of 1-[(2-Substituted phenyl)carbamoyl]naphthalen-2-yl Carbamates
JF - Molecules
VL - 21
IS - 9
PB - Mayer und Muller
SN - 14203049
KW - carbamates
KW - hydroxynaphthalene-carboxamides
KW - in vitro antibacterial activity
KW - in vitro antimycobacterial activity
KW - in vitro cytotoxicity assay
KW - structure-activity relationships
N2 - Series of thirteen 1-[(2-chlorophenyl)carbamoyl]naphthalen-2-yl carbamates and thirteen 1-[(2-nitrophenyl)carbamoyl]naphthalen-2-yl carbamates with alkyl/cycloalkyl/arylalkyl chains were prepared and characterized. Primary in vitro screening of the synthesized compounds was performed against Staphylococcus aureus, two methicillin-resistant S. aureus strains, Mycobacterium marinum, and M. kansasii. 1-[(2-Chlorophenyl)carbamoyl]naphthalen-2-yl ethylcarbamate and 1-[(2-nitrophenyl)carbamoyl]naphthalen-2-yl ethylcarbamate showed antistaphylococcal (MICs = 42 mu M against MRSA) and antimycobacterial (MICs = 21 mu M) activity against the tested strains comparable with or higher than that of the standards ampicillin and isoniazid. In the case of bulkier carbamate tails (R > propyl/isopropyl), the activity was similar (MICs ca. 70 mu M). Screening of the cytotoxicity of both of the most effective compounds was performed using THP-1 cells, and no significant lethal effect was observed (LD50 >30 mu M). The structure-activity relationships are discussed.
ER -
GONĚC, Tomáš, S POSPISILOVA, L HOLANOVA, J STRANIK, A CERNIKOVA, V PUDELKOVA, J KOS, M ORAVEC, Peter KOLLÁR, Alois ČÍŽEK a J JAMPILEK. Synthesis and Antimicrobial Evaluation of 1-[(2-Substituted phenyl)carbamoyl]naphthalen-2-yl Carbamates. \textit{Molecules}. BASEL: Mayer und Muller, 2016, roč.~21, č.~9, 15 s. ISSN~1420-3049. Dostupné z: https://dx.doi.org/10.3390/molecules21091189.
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