Investigating the activity spectrum for ring-substituted 8-hydroxyquinolines

研究环取代的 8-羟基喹啉的活性光谱

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作者:Robert Musiol, Josef Jampilek, Jacek E Nycz, Matus Pesko, James Carroll, Katarina Kralova, Marcela Vejsova, Jim O'Mahony, Aidan Coffey, Anna Mrozek, Jaroslaw Polanski

Abstract

In this study, a series of fourteen ring-substituted 8-hydroxyquinoline derivatives were prepared. The synthesis procedures 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 and against eight fungal strains. Several compounds showed biological activity comparable with or higher than the standards isoniazid or fluconazole. For all the compounds, the relationships between the lipophilicity and the chemical structure of the studied compounds are discussed.

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