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.
- MeSH
- antituberkulotika chemická syntéza chemie farmakologie MeSH
- atypické mykobakteriální infekce farmakoterapie MeSH
- bakteriální pneumonie farmakoterapie mikrobiologie MeSH
- chinazoliny chemická syntéza chemie farmakologie MeSH
- chloroplasty účinky léků MeSH
- fotosyntéza účinky léků MeSH
- lidé MeSH
- netuberkulózní mykobakterie účinky léků MeSH
- Spinacia oleracea účinky léků MeSH
- styreny chemická syntéza farmakologie MeSH
- transport elektronů účinky léků MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 2-styrylquinazolin-4(3H)-one MeSH Prohlížeč
- 4-chloro-2-styrylquinazoline MeSH Prohlížeč
- antituberkulotika MeSH
- chinazoliny MeSH
- styreny MeSH
- styrylquinazoline MeSH Prohlížeč
In the study, a series of twelve ring-substituted 4-hydroxy-1H-quinolin-2-one derivatives were prepared. The procedures for synthesis of the compounds are presented. The compounds were analyzed using RP-HPLC to determine lipophilicity and tested for their photosynthesis-inhibiting activity using spinach (Spinacia oleracea L.) chloroplasts. All the synthesized compounds were also evaluated for antifungal activity using in vitro screening with eight fungal strains. 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).
- MeSH
- antifungální látky chemie MeSH
- chinolony chemická syntéza farmakologie MeSH
- chloroplasty účinky léků MeSH
- fotosyntéza účinky léků MeSH
- houby účinky léků MeSH
- hydrofobní a hydrofilní interakce MeSH
- hydroxychinoliny chemická syntéza farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- antifungální látky MeSH
- chinolony MeSH
- hydroxychinoliny MeSH
