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Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues
Zentiva k.s., U kabelovny 130, 102 37 Prague 10, Czech Republic
Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1-3, 612 42 Brno, Czech Republic
Institute of Chemistry, University of Silesia, Szkolna 9, 40007 Katowice, Poland
Department of Ecosozology and Physiotactics, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia
Department of Biological Sciences, Cork Institute of Technology, Bishopstown, Cork, Ireland
Institute of Chemistry, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia
Department of Biological and Medical Sciences, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 500 05 Hradec Kralove, Czech Republic
* Author to whom correspondence should be addressed.
Received: 21 September 2009; in revised form: 13 October 2009 / Accepted: 21 October 2009 / Published: 23 October 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.
Keywords: styrylquinazolinone and styrylquinazoline derivatives; lipophilicity; PET inhibition; spinach chloroplasts; in vitro antimycobacterial activity; in vitro antifungal activity; structure-activity relationships
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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.
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(10):4246-4265.
Jampilek, Josef; Musiol, Robert; Finster, Jacek; Pesko, Matus; Carroll, James; Kralova, Katarina; Vejsova, Marcela; O'Mahony, Jim; Coffey, Aidan; Dohnal, Jiri; Polanski, Jaroslaw. 2009. "Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues." Molecules 14, no. 10: 4246-4265.