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@article{1413050,
author = {Gonec, Tomas and Kos, Jiri and Nevin, Eoghan and Govender, Rodney and Pesko, Matus and Tengler, Jan and Kushkevych, Ivan},
article_location = {Basel},
article_number = {7},
doi = {http://dx.doi.org/10.3390/molecules190710386},
keywords = {naphthalene; lipophilicity; in vitro antimycobacterial activity; in vitro cytotoxicity; photosynthetic electron transport inhibition; spinach chloroplasts},
language = {eng},
issn = {1420-3049},
journal = {Molecules},
note = {žádný z autorů nemá na WoS afiliaci na MU, nelze tedy výsledek přenášet do RIV!},
title = {Preparation and Biological Properties of Ring-Substituted Naphthalene-1-Carboxanilides},
url = {http://apps.webofknowledge.com/full_record.do?product=WOS&search_mode=GeneralSearch&qid=1&SID=F1crF62WD2aQBykkCNF&page=1&doc=10},
volume = {19},
year = {2014}
}
TY - JOUR
ID - 1413050
AU - Gonec, Tomas - Kos, Jiri - Nevin, Eoghan - Govender, Rodney - Pesko, Matus - Tengler, Jan - Kushkevych, Ivan
PY - 2014
TI - Preparation and Biological Properties of Ring-Substituted Naphthalene-1-Carboxanilides
JF - Molecules
VL - 19
IS - 7
SP - 10386-10409
EP - 10386-10409
PB - Mayer und Muller
SN - 14203049
N1 - žádný z autorů nemá na WoS afiliaci na MU, nelze tedy výsledek přenášet do RIV!
KW - naphthalene
KW - lipophilicity
KW - in vitro antimycobacterial activity
KW - in vitro cytotoxicity
KW - photosynthetic electron transport inhibition
KW - spinach chloroplasts
UR - http://apps.webofknowledge.com/full_record.do?product=WOS&search_mode=GeneralSearch&qid=1&SID=F1crF62WD2aQBykkCNF&page=1&doc=10
N2 - In this study, a series of twenty-two ring-substituted naphthalene-1-carboxanilides were prepared and characterized. Primary in vitro screening of the synthesized carboxanilides was performed against Mycobacterium avium subsp. paratuberculosis. N-(2-Methoxyphenyl) naphthalene-1-carboxamide, N-(3-methoxyphenyl) naphthalene-1-carboxamide, N-(3-methylphenyl) naphthalene-1-carboxamide, N-(4-methylphenyl) naphthalene-1-carboxamide and N-(3-fluorophenyl) naphthalene-1-carboxamide showed against M. avium subsp. paratuberculosis two-fold higher activity than rifampicin and three-fold higher activity than ciprofloxacin. The most effective antimycobacterial compounds demonstrated insignificant toxicity against the human monocytic leukemia THP-1 cell line. The testing of biological activity of the compounds was completed with the study of photosynthetic electron transport (PET) inhibition in isolated spinach (Spinacia oleracea L.) chloroplasts. The PET-inhibiting activity expressed by IC50 value of the most active compound N-[4-( trifluoromethyl) phenyl]naphthalene-1-carboxamide was 59 mu mol/L. The structure-activity relationships are discussed.
ER -
GONEC, Tomas, Jiri KOS, Eoghan NEVIN, Rodney GOVENDER, Matus PESKO, Jan TENGLER a Ivan KUSHKEVYCH. Preparation and Biological Properties of Ring-Substituted Naphthalene-1-Carboxanilides. \textit{Molecules}. Basel: Mayer und Muller, 2014, roč.~19, č.~7, s.~10386-10409. ISSN~1420-3049. Dostupné z: https://dx.doi.org/10.3390/molecules190710386.
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