Informace o publikaci

Preparation and Biological Properties of Ring-Substituted Naphthalene-1-Carboxanilides

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GONEC Tomas KOS Jiri NEVIN Eoghan GOVENDER Rodney PESKO Matus TENGLER Jan KUSHKEVYCH Ivan

Rok publikování 2014
Druh Článek v odborném periodiku
Časopis / Zdroj Molecules
Fakulta / Pracoviště MU

Přírodovědecká fakulta

Citace
www http://apps.webofknowledge.com/full_record.do?product=WOS&search_mode=GeneralSearch&qid=1&SID=F1crF62WD2aQBykkCNF&page=1&doc=10
Doi http://dx.doi.org/10.3390/molecules190710386
Klíčová slova naphthalene; lipophilicity; in vitro antimycobacterial activity; in vitro cytotoxicity; photosynthetic electron transport inhibition; spinach chloroplasts
Popis 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.

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