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Title: Investigating biological activity spectrum for novel styrylquinazoline analogues
Authors: Jampilek, J.
Musioł, Robert
Finster, Jacek
Pesko, M.
Carroll, J.
Kralova, K.
Vejsova, M.
O'Mahony, J.
Coffey, A.
Dohnal, J.
Polański, Jarosław
Keywords: In vitro antifungal activity; In vitro antimycobacterial activity; Lipophilicity; PET inhibition; Spinach chloroplasts; Structure-activity relationships; Styrylquinazolinone and styrylquinazoline derivatives
Issue Date: 2009
Citation: Molecules (Basel), vol. 14, iss. 10 (2009), s. 4246-4265
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.
DOI: 10.3390/molecules14104246
ISSN: 1420-3049
Appears in Collections:Artykuły (WNŚiT)

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