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Investigating biological activity spectrum for novel styrylquinazoline analogues
J. Jampílek, R. Musiol, J. Finster, M. Peško, J. Carroll, K. Kráľová, M. Vejsová, J. O'Mahony, A. Coffey, J. Dohnal, J. Polanski
Jazyk angličtina Země Švýcarsko
Typ dokumentu práce podpořená grantem
E-zdroje NLK Online
Directory of Open Access Journals od 1997Free Medical Journals od 1997
PubMed Central od 2001
Europe PubMed Central od 2001
ProQuest Central od 1997-01-01
Open Access Digital Library od 1997-01-01
Medline Complete (EBSCOhost) od 2009-03-01
Health & Medicine (ProQuest) od 1997-01-01
- MeSH
- antituberkulotika farmakologie chemická syntéza chemie MeSH
- atypické mykobakteriální infekce farmakoterapie MeSH
- bakteriální pneumonie farmakoterapie mikrobiologie MeSH
- chinazoliny farmakologie chemická syntéza chemie MeSH
- chloroplasty účinky léků MeSH
- fotosyntéza účinky léků MeSH
- lidé MeSH
- netuberkulózní mykobakterie účinky léků MeSH
- Spinacia oleracea účinky léků MeSH
- styreny farmakologie chemická syntéza MeSH
- transport elektronů účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- práce podpořená grantem MeSH
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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- $a 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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