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Usage Statistics Cite this paper as: Musiol, R.; Jampilek, J.; Pesko, M.; Carroll, J.; Kralova, K.; Finster, J.; O'Mahony, J.; Coffey, A.; Polanski, J. Substituted 2-Styrylquinazoline Derivatives: Preparation and Their Biological Activities. In Proceedings of the 13th Int. Electron. Conf. Synth. Org. Chem., 1-30 November 2009; Sciforum Electronic Conferences Series, 2009, c004:1-12.
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13th Int. Electron. Conf. Synth. Org. Chem. 2009, c004:1-12
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Substituted 2-Styrylquinazoline Derivatives: Preparation and Their Biological Activities
Robert Musiol 1,* 
, Josef Jampilek 2,3,* , Matus Pesko 4, James Carroll 5, Katarina Kralova 6, Jacek Finster 1, Jim O'Mahony 5, Aidan Coffey 5 and Jaroslaw Polanski 1
, Josef Jampilek 2,3,* , Matus Pesko 4, James Carroll 5, Katarina Kralova 6, Jacek Finster 1, Jim O'Mahony 5, Aidan Coffey 5 and Jaroslaw Polanski 11 Institute of Chemistry, University of Silesia, Szkolna 9, 40007 Katowice, Poland;
2 Zentiva a.s., U kabelovny 130, 102 37 Prague 10, Czech Republic;
3 Department of Chemical Drugs, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Palackeho 1/3, 61242 Brno, Czech Republic;
4 Department of Ecosozology and Physiotactics, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia;
5 Department of Biological Sciences, Cork Institute of Technology, Bishopstown, Cork, Ireland;
6 Institute of Chemistry, Faculty of Natural Sciences, Comenius University, Mlynska dolina Ch-2, 84215 Bratislava, Slovakia;
* Author to whom correspondence should be addressed.
(This article belongs to the section C. Bioorganic Chemistry and Natural Products)
Abstract: In this study, a series of five ring-substituted 2-styrylquinazolin-4(3H)-one and five ring-substituted 4-chloro-2-styrylquinazoline derivatives were prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity. They were tested for their activity related to inhibition of 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. Several compounds showed biological activity comparable with or higher than the standard isoniazid. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed, as well as their structure-activity relationships (SAR).
Keywords: Styrylquinazoline derivatives; Lipophilicity; PET inhibition; Spinach chloroplasts; In vitro antimycobacterial activity; Structure-activity relationships
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