1,3,4-[口恶]二唑类化合物的合成及生物活性研究进展  

Research Progress in the Syntheses and Biological Activities of 1,3,4-Oxadiazole Compounds

作　　者：杨碧蓉 邰晔弘 王玉梨 王顺优 张海珍 杨岚 YANG Bi-rong;TAI Ye-hong;WANG Yu-li;WANG Shun-you;ZHANG Hai-zhen;YANG Lan(College of Pharmacy,Guizhou University,Guiyang 550025,China;Engineering Laboratory for Synthetic Drugs,Guizhou University,Guiyang 550025,China;Guizhou Lianda Testing Technology Co.,Ltd.,Guiyang 550025,China)

机构地区：[1]贵州大学药学院,贵州贵阳550025 [2]贵州大学贵州省合成药物工程实验室,贵州贵阳550025 [3]贵州省联大检测技术有限公司,贵州贵阳550025

出　　处：《化学试剂》2024年第3期24-32,共9页Chemical Reagents

基　　金：大学生创新创业训练计划项目(贵大(校)创字(2022)028号);贵州大学2023年实验室开放项目(SYSKF2023-096)。

摘　　要：1,3,4-[口恶]二唑是一类重要的含氮五元芳香杂环类结构单元,可与多种药效团融合,产生不同的生物活性,因此引起了人们的关注,也显示了广泛的应用和发展前景,在医药和农药领域尤为突出。综述了国内外以酰肼环合法、Huisgen反应高效构建1,3,4-[口恶]二唑类化合物的方法,同时对1,3,4-[口恶]二唑类化合物在抗病毒、抗菌、抗肿瘤、除草、杀虫等方面的生物活性进行了介绍,并对各类化合物的构效关系进行总结,为进一步研究1,3,4-[口恶]二唑类化合物的设计合成及其生物活性提供参考和借鉴。1,3,4-oxadiazoles are important class of nitrogen-containing five-membered aromatic heterocyclic structural unit,which can produce a variety of biological activities after combining with multi kinds of pharmacophore,so many compounds containing 1,3,4-oxadiazoles core structure have attracted people's attention and show a wide application and development prospects,especially in the field of medicine and agriculture.The efficient construction of 1,3,4-oxadiazole compounds by hydrazide ring method and Huisgen reaction,meanwhile,the biological activities of 1,3,4-oxadiazole such as antiviral,antibacterial,antitumor,herbicidal and insecticidal and so on have been introduced,and summarized the structure-activity relationship of various compounds.It provides reference and guidance for further study on the design,synthesis and biological activities of 1,3,4-oxadiazole compounds.

关 键 词：1 3 4-[口恶]二唑 合成 药效团融合 生物活性 研究进展 

分 类 号：O626.24[理学—有机化学]