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Molecules 2009, 14(10), 4246-4265; doi:10.3390/molecules14104246
Article

Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues

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Received: 21 September 2009 / Revised: 13 October 2009 / Accepted: 21 October 2009 / Published: 23 October 2009
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Abstract

In this study, series of ring-substituted 2-styrylquinazolin-4(3H)-one and 4-chloro-2-styrylquinazoline derivatives were prepared. The syntheses of the discussed compounds are presented. The compounds were analyzed by RP-HPLC to determine lipophilicity. They were tested for their inhibitory activity on photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial strains and against eight fungal strains. Several compounds showed biological activity comparable with or higher than that of the standard isoniazid. It was found that the electronic properties of the R substituent, and not the total lipophilicity of the compound, were decisive for the photosynthesis-inhibiting activity of tested compounds.
Keywords: styrylquinazolinone and styrylquinazoline derivatives; lipophilicity; PET inhibition; spinach chloroplasts; in vitro antimycobacterial activity; in vitro antifungal activity; structure-activity relationships styrylquinazolinone and styrylquinazoline derivatives; lipophilicity; PET inhibition; spinach chloroplasts; in vitro antimycobacterial activity; in vitro antifungal activity; structure-activity relationships
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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Jampilek, J.; Musiol, R.; Finster, J.; Pesko, M.; Carroll, J.; Kralova, K.; Vejsova, M.; O'Mahony, J.; Coffey, A.; Dohnal, J.; Polanski, J. Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues. Molecules 2009, 14, 4246-4265.

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