Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities
Synthesis of neamine-carboline conjugates for RNA binding and their antibacterial activities
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用于RNA结合的新胺-咔啉缀合物的合成及其抗菌活性
DOI：
10.1016/j.tet.2010.03.034
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发表时间：
2010-05-08
期刊：
影响因子：
2.1
通讯作者：
Ye, Xin-Shan
中科院分区：
文献类型：
--
作者：
Wu, Shan;Fu, Yunsha;Ye, Xin-Shan
以脂肪族二胺为连接基，将新霉胺与β-咔啉-3-羧酸偶联，合成了3种新霉胺-β-咔啉偶联物，并利用表面等离子体共振（SPR）技术研究了偶联物与16 SrRNA和18 SrRNA的结合特性，结果表明，部分偶联物与新霉胺的结合能力较强。体外抗菌活性测试结果表明，部分合成化合物的抗菌活性优于新霉胺。初步探讨了构效关系。实验结果表明，合成的新霉胺-咔啉偶联物具有作为新抗生素的潜力。(C)2010爱思唯尔有限公司版权所有。
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.