新型磺胺类喹唑啉衍生物的设计、合成及抗病毒活性评价

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Accounts of Chemical Research Pub Date : 2023-01-01 DOI:10.1515/hc-2022-0160

Yixiang Deng, Shitao Yin, Xinyun Jing, Yu-Tao Zheng

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引用次数: 0

摘要

摘要设计合成了一系列新的含有磺酰胺部分的喹唑啉衍生物，并用1H NMR、13C NMR和HRMS技术对其结构进行了表征。其中，通过X射线单晶衍射分析进一步证实了化合物E1的结构。采用半叶法对其抗烟草花叶病毒（TMV）活性进行了评价。生物测定结果表明，E8和E19对TMV具有良好的抑制活性。E8和E19的治疗活性、保护活性和灭活活性的EC50分别为132.1、152.8、57.4 mg/L和278.0165.394.5 mg/L，远远优于利巴韦林（318.2201.5128.6 mg/L）。

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Design, synthesis, and antiviral activities evaluation of novel quinazoline derivatives containing sulfonamide moiety

Abstract A series of novel quinazoline derivatives bearing sulfonamide moiety was designed and synthesized, and their structure were characterized by 1H NMR, 13C NMR, and HRMS techniques. Among them, the structure of compound E1 was further confirmed through X-ray single-crystal diffraction analyses. Their anti-Tobacco mosaic virus (TMV) activities were evaluated through half-leaf method. The bioassay results showed that E8 and E19 possess excellent inhibitory activity towards TMV. The EC50 of curative activities, protective activities, and inactivating activities of E8 and E19 are 132.1, 152.8, 57.4 mg/L and 278.0, 165.3, 94.5 mg/L, respectively, which are far superior than Ribavirin (318.2, 201.5, 128.6 mg/L, respectively).

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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.