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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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