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Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues (2009)

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.

Publication details
Download http://www.mdpi.com/1420-3049/14/10/4246/
http://www.doaj.org/doaj?func=openurl&genre=article&issn=14203049&date=2009&volume=14&issue=10&spage=4246
Publisher Molecular Diversity Preservation International
Repository DOAJ-Articles (Sweden)
Keywords styrylquinazolinone and styrylquinazoline derivatives, lipophilicity, PET inhibition, spinach chloroplasts, in vitro antimycobacterial activity, in vitro antifungal activity, structure-activity relationships
Language eng