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学科主题: 药学
题名:
Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities
作者: 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
发表日期: 2010-05-08
DOI: 10.1016/j.tet.2010.03.034
卷: 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
所属项目编号: 973
项目资助者: National Natural Science Foundation of China ; Ministry of Science and Technology of China
WOS记录号: WOS:000277967400007
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/53921
Appears in Collections:北京大学药学院_期刊论文

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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

Recommended Citation:
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.
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