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环取代的4-羟基-1H-喹啉-2-酮:制备与生物活性。

Ring-substituted 4-hydroxy-1H-quinolin-2-ones: preparation and biological activity.

作者信息

Jampilek Josef, Musiol Robert, Pesko Matus, Kralova Katarina, Vejsova Marcela, Carroll James, Coffey Aidan, Finster Jacek, Tabak Dominik, Niedbala Halina, Kozik Violetta, Polanski Jaroslaw, Csollei Jozef, Dohnal Jiri

机构信息

Zentiva ks, U Kabelovny 130, Prague 10, Czech Republic.

出版信息

Molecules. 2009 Mar 13;14(3):1145-59. doi: 10.3390/molecules14031145.

Abstract

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).

摘要

在该研究中,制备了一系列十二个环取代的4-羟基-1H-喹啉-2-酮衍生物。介绍了这些化合物的合成步骤。使用反相高效液相色谱法(RP-HPLC)分析这些化合物以测定亲脂性,并使用菠菜(Spinacia oleracea L.)叶绿体测试它们的光合作用抑制活性。还使用八种真菌菌株进行体外筛选,对所有合成化合物的抗真菌活性进行了评估。针对所有化合物,讨论了所研究化合物的亲脂性与化学结构之间的关系,以及它们的构效关系(SAR)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/076d/6253998/39f6c0229f27/molecules-14-01145-g003.jpg

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