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Molecules 2010, 15(11), 8122-8142; doi:10.3390/molecules15118122
Article

Investigating the Spectrum of Biological Activity of Ring-Substituted Salicylanilides and Carbamoylphenylcarbamates

1, 1,2, 3, 4, 5, 5, 6, 7, 7, 4, 1, 7 and 1,2,*
Received: 13 August 2010; in revised form: 5 November 2010 / Accepted: 9 November 2010 / Published: 10 November 2010
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Abstract: In this study, a series of twelve ring-substituted salicylanilides and carbamoylphenylcarbamates were prepared and characterized. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Moreover, their site of action in the photosynthetic apparatus was determined. Primary in vitro screening of the synthesized compounds was also performed against mycobacterial, bacterial and fungal strains. Several compounds showed biological activity comparable with or higher than the standards 3-(3,4-dichlorophenyl)-1,1-dimethylurea, isoniazid, penicillin G, ciprofloxacin or fluconazole. The most active compounds showed minimal anti-proliferative activity against human cells in culture, indicating they would have low cytotoxicity. For all compounds, the relationships between lipophilicity and the chemical structure are discussed.
Keywords: salicylanilides; lipophilicity; EPR study; photosynthetic electron transport inhibition; spinach chloroplasts; in vitro anti-fungal activity; in vitro anti-bacterial activity; in vitro anti-mycobacterial activity; anti-proliferative activity   salicylanilides; lipophilicity; EPR study; photosynthetic electron transport inhibition; spinach chloroplasts; in vitro anti-fungal activity; in vitro anti-bacterial activity; in vitro anti-mycobacterial activity; anti-proliferative activity  
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Otevrel, J.; Mandelova, Z.; Pesko, M.; Guo, J.; Kralova, K.; Sersen, F.; Vejsova, M.; Kalinowski, D.S.; Kovacevic, Z.; Coffey, A.; Csollei, J.; Richardson, D.R.; Jampilek, J. Investigating the Spectrum of Biological Activity of Ring-Substituted Salicylanilides and Carbamoylphenylcarbamates. Molecules 2010, 15, 8122-8142.

AMA Style

Otevrel J, Mandelova Z, Pesko M, Guo J, Kralova K, Sersen F, Vejsova M, Kalinowski DS, Kovacevic Z, Coffey A, Csollei J, Richardson DR, Jampilek J. Investigating the Spectrum of Biological Activity of Ring-Substituted Salicylanilides and Carbamoylphenylcarbamates. Molecules. 2010; 15(11):8122-8142.

Chicago/Turabian Style

Otevrel, Jan; Mandelova, Zuzana; Pesko, Matus; Guo, Jiahui; Kralova, Katarina; Sersen, Frantisek; Vejsova, Marcela; Kalinowski, Danuta S.; Kovacevic, Zaklina; Coffey, Aidan; Csollei, Jozef; Richardson, Des R.; Jampilek, Josef. 2010. "Investigating the Spectrum of Biological Activity of Ring-Substituted Salicylanilides and Carbamoylphenylcarbamates." Molecules 15, no. 11: 8122-8142.



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