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三唑和恶二唑嘧啶杂化物及其核苷类似物的合成与抗H5N1病毒活性

Synthesis and anti-H5N1 virus activity of triazole- and oxadiazole-pyrimidine hybrids and their nucleoside analogs.

作者信息

Tolan Hala E M, El-Sayed Wael A, Tawfek Nashwa, Abdel-Megeid Farouk M E, Kutkat Omnya M

机构信息

Photochemistry Department, National Research Centre, Dokki, Giza, Egypt.

Chemistry Department, Faculty of Science, Qassim University, Kingdom of Saudi Arabia.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2020;39(5):649-670. doi: 10.1080/15257770.2019.1674331. Epub 2019 Oct 10.

Abstract

New 1,2,3-triazole glycosides and 1,2,4-thioglycosides incorporating a substituted pyrimidinedione ring system were synthesized via click dipolar cycloaddition and heterocyclization of hydrazine-1-carbodithioate derivatives, respectively. The sugar hydrazine derivatives linked aminodimethyluracil were also prepared. In addition, the oxadiazoline substituted with acyclic sugar moieties linked to the pyrimidinedione as acyclic nucleoside analogs were synthesized. The antiviral activity of the synthesized compounds against avian influenza H5N1 virus was investigated and compounds , and showed good activities against the virus strains.

摘要

分别通过点击偶极环加成反应和肼-1-碳二硫代酸酯衍生物的杂环化反应,合成了含有取代嘧啶二酮环系统的新型1,2,3-三唑糖苷和1,2,4-硫代糖苷。还制备了连接氨基二甲基尿嘧啶的糖肼衍生物。此外,合成了作为无环核苷类似物与嘧啶二酮相连的带有无环糖部分的恶二唑啉。研究了合成化合物对禽流感H5N1病毒的抗病毒活性,化合物 、 和 对病毒株表现出良好的活性。

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