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Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues

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...

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Autores principales: Jampilek, Josef, Musiol, Robert, Finster, Jacek, Pesko, Matus, Carroll, James, Kralova, Katarina, Vejsova, Marcela, O'Mahony, Jim, Coffey, Aidan, Dohnal, Jiri, Polanski, Jaroslaw
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International 2009
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6254837/
https://www.ncbi.nlm.nih.gov/pubmed/19924061
http://dx.doi.org/10.3390/molecules14104246
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author Jampilek, Josef
Musiol, Robert
Finster, Jacek
Pesko, Matus
Carroll, James
Kralova, Katarina
Vejsova, Marcela
O'Mahony, Jim
Coffey, Aidan
Dohnal, Jiri
Polanski, Jaroslaw
author_facet Jampilek, Josef
Musiol, Robert
Finster, Jacek
Pesko, Matus
Carroll, James
Kralova, Katarina
Vejsova, Marcela
O'Mahony, Jim
Coffey, Aidan
Dohnal, Jiri
Polanski, Jaroslaw
author_sort Jampilek, Josef
collection PubMed
description 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.
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spelling pubmed-62548372018-11-30 Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues Jampilek, Josef Musiol, Robert Finster, Jacek Pesko, Matus Carroll, James Kralova, Katarina Vejsova, Marcela O'Mahony, Jim Coffey, Aidan Dohnal, Jiri Polanski, Jaroslaw Molecules Article 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. Molecular Diversity Preservation International 2009-10-23 /pmc/articles/PMC6254837/ /pubmed/19924061 http://dx.doi.org/10.3390/molecules14104246 Text en © 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Jampilek, Josef
Musiol, Robert
Finster, Jacek
Pesko, Matus
Carroll, James
Kralova, Katarina
Vejsova, Marcela
O'Mahony, Jim
Coffey, Aidan
Dohnal, Jiri
Polanski, Jaroslaw
Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues
title Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues
title_full Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues
title_fullStr Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues
title_full_unstemmed Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues
title_short Investigating Biological Activity Spectrum for Novel Styrylquinazoline Analogues
title_sort investigating biological activity spectrum for novel styrylquinazoline analogues
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6254837/
https://www.ncbi.nlm.nih.gov/pubmed/19924061
http://dx.doi.org/10.3390/molecules14104246
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