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Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities
Wu, Shan; Fu, Yunsha; Yan, Ribai; Wu, Yanfen1; Lei, Xiaoping; Ye, Xin-Shan
关键词Aminoglycoside Beta-carboline Rna Binding Antibacterial Activity Synthesis
刊名TETRAHEDRON
2010-05-08
DOI10.1016/j.tet.2010.03.034
66期:19页:3433-3440
收录类别SCI ; IC
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]16S RIBOSOMAL-RNA ; SURFACE-PLASMON RESONANCE ; TARGETING RNA ; NEOMYCIN-B ; AMINOGLYCOSIDE MIMETICS ; ANTIBIOTICS ; DESIGN ; SITE ; RECOGNITION ; DERIVATIVES
英文摘要

Three types of neamine-beta-carboline conjugates were synthesized in good yields by the coupling of neamine and beta-carboline-3-carboxylic acids using aliphatic diamine as a linker, The binding properties of these conjugates to 16S rRNA and 18S rRNA were evaluated by surface plasmon resonance (SPR), showing that some conjugates had stronger binding affinities than neamine. In vitro antimicrobial activities were also evaluated and the results showed that some synthetic compounds exhibited better antibacterial activities than neamine. The preliminary structure-activity relationship was discussed. The present experimental data demonstrated that synthetic neamine-carboline conjugates might hold the potential as new antibiotics. (C) 2010 Elsevier Ltd. All rights reserved.

语种英语
WOS记录号WOS:000277967400007
项目编号973
资助机构National Natural Science Foundation of China ; Ministry of Science and Technology of China
引用统计
被引频次:11[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/53921
专题北京大学药学院
北京大学药学院_药物化学系
作者单位1.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
2.Peking Univ, Sch Pharmaceut Sci, Beijing 100191, Peoples R China
推荐引用方式
GB/T 7714
Wu, Shan,Fu, Yunsha,Yan, Ribai,et al. Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities[J]. TETRAHEDRON,2010,66(19):3433-3440.
APA Wu, Shan,Fu, Yunsha,Yan, Ribai,Wu, Yanfen,Lei, Xiaoping,&Ye, Xin-Shan.(2010).Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities.TETRAHEDRON,66(19),3433-3440.
MLA Wu, Shan,et al."Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities".TETRAHEDRON 66.19(2010):3433-3440.
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