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新型含 1,2,3-噻二唑和 1,3,4-噁二唑/噻二唑部分的硫醚/砜衍生物的合成及生物活性。

Synthesis and bioactivities of novel thioether/sulfone derivatives containing 1,2,3-thiadiazole and 1,3,4-oxadiazole/thiadiazole moiety.

机构信息

Center for Research and Development of Fine Chemicals, State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, PR China.

出版信息

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5821-4. doi: 10.1016/j.bmcl.2013.08.107. Epub 2013 Sep 6.

Abstract

A series of new thioether/sulfone compounds containing 1,2,3-thiadiazole and 1,3,4-oxadiazole/1,3,4-thiadiazole moiety were synthesized, the structures of all products were confirmed by IR, (1)H NMR, (13)C NMR, and element analysis. Preliminary antifungal activity test showed that compound 8a exhibited moderate antifungal activity against Fusarium oxysporum at 50μg/mL. Preliminary antiviral activity results showed that compounds 7a, 7c, 7d, 8a, and 9a displayed high antiviral activity against tobacco mosaic virus. The present work demonstrates that thioether/sulfone heterocyclic derivatives could be considered as new lead compounds for antiviral studies.

摘要

一系列含有 1,2,3-噻二唑和 1,3,4-噁二唑/1,3,4-噻二唑部分的新型硫醚/砜化合物被合成出来,所有产物的结构均通过 IR、(1)H NMR、(13)C NMR 和元素分析得到确认。初步的抗真菌活性测试表明,化合物 8a 在 50μg/mL 时对尖孢镰刀菌表现出中等的抗真菌活性。初步的抗病毒活性结果表明,化合物 7a、7c、7d、8a 和 9a 对烟草花叶病毒表现出高抗病毒活性。本工作表明,硫醚/砜杂环衍生物可被视为抗病毒研究的新型先导化合物。

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