Institute of Chemistry, University of Silesia, Szkolna 9, 40007 Katowice, Poland.
Molecules. 2010 Jan 12;15(1):288-304. doi: 10.3390/molecules15010288.
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.
在这项研究中，制备了一系列十四种环取代的 8-羟基喹啉衍生物。给出了合成步骤。利用反相高效液相色谱法（RP-HPLC）分析了这些化合物的亲脂性。测试了它们在菠菜（Spinacia oleracea L.）叶绿体中抑制光合作用电子传递（PET）活性的相关性质。还对合成的化合物进行了针对四种分枝杆菌菌株和八种真菌菌株的初步体外筛选。一些化合物表现出与标准异烟肼或氟康唑相当或更高的生物活性。对于所有化合物，都讨论了其亲脂性与所研究化合物的化学结构之间的关系。
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