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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...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Molecular Diversity Preservation International
2009
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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. |
format | Online Article Text |
id | pubmed-6254837 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2009 |
publisher | Molecular Diversity Preservation International |
record_format | MEDLINE/PubMed |
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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