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

IF 1.3 3区化学 Q3 CHEMISTRY, ORGANIC

Heterocyclic Communications Pub Date : 2023-01-01 DOI:10.1515/hc-2022-0160

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

引用次数: 0

Abstract

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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新型磺胺类喹唑啉衍生物的设计、合成及抗病毒活性评价

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）。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Heterocyclic Communications 化学-有机化学

CiteScore

3.80

自引率

4.30%

发文量

审稿时长

1.4 months

期刊介绍： Heterocyclic Communications (HC) is a bimonthly, peer-reviewed journal publishing preliminary communications, research articles, and reviews on significant developments in all phases of heterocyclic chemistry, including general synthesis, natural products, computational analysis, considerable biological activity and inorganic ring systems. Clear presentation of experimental and computational data is strongly emphasized. Heterocyclic chemistry is a rapidly growing field. By some estimates original research papers in heterocyclic chemistry have increased to more than 60% of the current organic chemistry literature published. This explosive growth is even greater when considering heterocyclic research published in materials science, physical, biophysical, analytical, bioorganic, pharmaceutical, medicinal and natural products journals. There is a need, therefore, for a journal dedicated explicitly to heterocyclic chemistry and the properties of heterocyclic compounds.