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喹喔啉酮作为药物研发中的优势平台。

Quinoxalinone as a Privileged Platform in Drug Development.

作者信息

Shi Leilei, Hu Wei, Wu Jifeng, Zhou Huaiyu, Zhou Hua, Li Xun

机构信息

Key Laboratory of Chemistry and Chemical Biology (Ministry of Education), Department of Pharmaceutical Science, College of Pharmacy, Shandong University, Jinan, China.

State Key Laboratory of Microbial Technology, School of Life Science, Shandong University, Ji'nan, China.

出版信息

Mini Rev Med Chem. 2018 Feb 14;18(5):392-413. doi: 10.2174/1389557517666171101111134.

Abstract

Among the family of nitrogen-containing heterocycles, quinoxalinone (or quinoxalin-2-one) core, characterized by pyrazin-2(1H)-one fused to benzene ring at two adjacent carbon atoms, has been frequently found in a variety of pharmacologically active compounds with biological or pharmaceutical applications. It was gratifying that a larger part of these bioactive quinoxalinone-based derivatives has entered various clinical trials, which in turn hastens the synthetic versatility and also initiates various derivatization of quinoxalinone scaffold. In this review, we highlighted the newly emerged quinoxalinone- based derivatives or analogues, with the emphasis of their biological applications and structure-activity analysis covering literatures in recent years.

摘要

在含氮杂环化合物家族中,喹喔啉酮(或喹喔啉 -2- 酮)核心结构,其特征是吡嗪 -2(1H)- 酮在两个相邻碳原子处与苯环稠合,在具有生物或药物应用的多种药理活性化合物中经常被发现。令人欣慰的是,这些基于喹喔啉酮的生物活性衍生物中的很大一部分已进入各种临床试验,这反过来又促进了合成的多样性,并引发了喹喔啉酮骨架的各种衍生化。在本综述中,我们重点介绍了新出现的基于喹喔啉酮的衍生物或类似物,重点是它们的生物学应用以及近年来文献中的构效关系分析。

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