新型氟化菲啶-6(5H)-酮衍生物的高效合成及其抗病毒活性的体外评估

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Accounts of Chemical Research Pub Date : 2024-01-06 DOI:10.1016/j.jfluchem.2024.110240

Larisa Gurskaya , Larisa Politanskaya , Jiaying Wang , Polina Ilyina , Alexandrina Volobueva , Vladimir Zarubaev

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引用次数: 0

摘要

本研究介绍了一种在氯苯中以三氟甲磺酸为介质，从相应的 2-异氰酸基-1,1′-联苯合成氟化菲啶-6(5H)-酮的便捷而高效的方法。该反应使用现成的起始材料，在非常温和的反应条件（r. t. ）下进行，可以获得具有生物前景的氟化杂环，收率良好甚至极佳。合成的化合物在 MDCK 细胞系中进行了细胞毒性体外测试，并对 A/波多黎各/8/34（H1N1）流感病毒进行了抗病毒活性测试。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Efficient synthesis of novel fluorinated phenanthridin-6(5H)-one derivatives and in vitro evaluation of their antiviral activity

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Efficient synthesis of novel fluorinated phenanthridin-6(5H)-one derivatives and in vitro evaluation of their antiviral activity

A convenient and efficient method for the synthesis of fluorinated phenanthridin-6(5H)-ones from the corresponding 2-isocyanato-1,1′-biphenyls mediated by trifluoromethanesulfonic acid in chlorobenzene is described. The reaction uses readily available starting materials, takes place under very mild reaction conditions (r. t.) and provides access to biologically promising fluorinated heterocycles in good to excellent yields. Synthesized compounds were tested in vitro for cytotoxicity in MDCK cell line and for antiviral activity against influenza virus A/Puerto Rico/8/34 (H1N1).

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来源期刊

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.