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Investigating Spectrum of Biological Activity of 4- and 5-Chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoethyl]benzamides.
Authors: Imramovský Aleš | Peško M | Králová K | Vejsová M | Stolaříková J | Vinšová J | Jampílek J
Year: 2011
Type of publication: článek v odborném periodiku
Name of source: Molecules
Publisher name: Molecular Diversity Preservation International
Place: Basel
Page from-to: 2414-2430
Titles:
Language Name Abstract Keywords
cze Výzkum biologické aktivity 4- a 5-Chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoetyl]benzamidů V této studii byla studována serie 22 5-Chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoetyl]benzamidů a 10 4-Chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoetyl]benzamidů. Lipofilita sloučenin byla stanovena RP-HPLC. Primární testování sloučenin bylo provedeno proti mykobakteriálním, bakteriálním a fugálním kmenům. Látky byly také testovány pro zjištění jejich schopnosti inhibovat elektron transport při fotosyntéze v chloroplastech špenátu (Spinacia oleracea L.). Sloučeniny vykázaly při jednotlivých testech srovnatelnou nebo vyšší než standardní léčiva isoniazid, flukonazol, penicillin G or ciprofloxacin. Pro všechny sloučeniny bylo provedeno srovnání lipofility a chemické struktury stejně tak ve srovnání s biologickou aktivitou. salicylanilid deriváty;lipofilita;chloroplasty špenátu
eng Investigating Spectrum of Biological Activity of 4- and 5-Chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoethyl]benzamides. In this study, a series of twenty-two 5-chloro-2-hydroxy-N-[2-(arylamino)-1- alkyl-2-oxoethyl]benzamides and ten 4-chloro-2-hydroxy-N-[2-(arylamino)-1-alkyl-2-oxoethyl]benzamides is described. The compounds were analyzed using RP-HPLC to determine lipophilicity. Primary in vitro screening of the synthesized compounds was performed against mycobacterial, bacterial and fungal strains. They were also evaluated for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. The compounds showed biological activity comparable with or higher than the standards isoniazid, fluconazole, penicillin G or ciprofloxacin. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds as well as their structure-activity relationships are discussed. salicylanilide derivates;lipophilicity;in vitro antimycobacterial activity;in vitro antifungal activity;in vitro antibacterial activity;PET inhibition;spinach chloroplasts;structure–activity relationships

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