共查询到20条相似文献,搜索用时 109 毫秒
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核苷类似物可以参与并干扰细菌(病毒)的DNA或RNA过程,抑制其生长和繁殖,从而有希望发展为抗肿瘤抗病毒药物。一些天然的核苷化合物虽然表现出一定的生理活性,在体内缺乏酶稳定性和靶向选择性却限制了其在医药领域的应用,合成具有生物活性的化学修饰的核苷及其衍生物是核酸药物化学中的重要课题。一类在金属卡宾复合物催化下的分子内或分子间烯烃重组反应-----复分解反应的发展使核苷类似物的合成进入了新阶段, 烯烃复分解反应成为核苷类似物合成的主要途径之一。随着施洛克催化剂、格拉布催化剂等复分解反应催化剂的发现和不断改进,烯烃复分解反应,尤其是关环复分解和交叉复分解反应被广泛应用于构建核苷类似物的糖环(或伪糖)结构或连接核苷类似物单体而形成核苷多聚物。本文对烯烃复分解反应在核苷类似物包括碳环核苷,2’,3’-双脱氧核苷,无环核苷,多环核苷及核苷二聚体或三聚体的合成中的应用进行了综述。 相似文献
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研究了有机溶剂中酶促核苷类化合物3'-酯高区域选择性的合成反应,探讨了核苷结构中R1位取代基变化对酶促酰化反应的影响.结果表明:来源于Burkholderia cepacia的固定化脂肪酶PS IM在有机溶剂THF中的催化效果最佳,且酰化反应的优势位点均为3'-羟基(90%~>99%);随着核苷中R1位取代基由F变化至CF3或酰基供体链长由C6增加至C14,该酰化反应的3'-区域选择性均呈现逐渐增加的趋势,构效关系分析表明,这主要源于PS IM酶特殊的活性中心结构. 相似文献
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研究了有机溶剂中酶促核苷类化合物3'-酯高区域选择性的合成反应,探讨了核苷结构中R1位取代基变化对酶促酰化反应的影响.结果表明:来源于Burkholderia cepacia的固定化脂肪酶PS IM在有机溶剂THF中的催化效果最佳,且酰化反应的优势位点均为3'-羟基(90%~>99%);随着核苷中R1位取代基由F变化至CF3或酰基供体链长由C6增加至C14,该酰化反应的3'-区域选择性均呈现逐渐增加的趋势,构效关系分析表明,这主要源于PS IM 酶特殊的活性中心结构. 相似文献
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含酰基氨基甲酸酯基硫脲核苷类化合物的合成及生物活性 总被引:3,自引:0,他引:3
在前期核苷类化合物的研究基础之上,为了进一步改善该类化合物的生物活性,基于几丁质合成酶催化作用机制,通过活性亚结构拼接方法,将具有良好生物活性的氨基甲酸酯基片段引入到前期所设计化合物的硫脲桥当中,设计合成了一系列结构新颖的含酰基氨基甲酸酯基硫脲的核苷类化合物.以尿苷为原料,经4步反应制得目标物,其结构经IR,1H NMR及HRMS确证.初步生测结果表明,部分化合物具有一定的杀菌和杀虫活性,化合物5j对棉铃虫的抑制活性与对照药剂除虫脲相当. 相似文献
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Sophie Danappe Fabien Boeda Christian Alexandre Anne‐Marie Aubertin Nathalie Bourgougnon 《合成通讯》2013,43(21):3225-3239
Synthesis of eight nucleoside analogues 4–11 with a methylenecyclobutane unit is described. Wittig reaction with 2‐hydroxymethylcyclobutanone 12 gave a mixture of Z (13) and E (14) derivatives, which was separated before functional modifications. The heterocyclic moieties were introduced via a Mitsunobu reaction either on the saturated chain or on the unsaturated chain. When adenine was used in this reaction, only the N‐9 substitution products were obtained. Removal of the protecting groups provided the target products. 相似文献
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IntroductionNucleosidesandtheiranaloguesaspotentialanti cancerandantivirusagentshavebeenstudiedextensively .Mostofthecurrentlylicensedantiviraldrugsandmanyofthedrugsusedinanticancerchemotherapyarenucleosideanalogues .1Forthemajorityoftheseanaloguesshown… 相似文献
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Novel 1,3-dioxolane C-nucleoside analogues of tiazofurin 2-(2-hydroxymethyl-1,3-dioxolan-4-yl)-1,3-thiazole4-carboxamide as well as N-nucleoside analogues of substituted imidazoles 1-(2-hydroxymethyl-1,3-dioxolan4-yl)-4-nitroimidazole and 1-(2-hydroxymethyl-1,3-dioxolan-4-yl)-4,5-dicyanoimidazole were synthesized from methyl acrylate through a multistep procedure. Their structures were confirmed by IR,^1H NMR,^13C NMR spectraand elemental analysis. 相似文献
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采用微波法,取代苯甲醛分别与环戊酮和环己酮经克莱森-斯密特缩合反应制得中间体2,6-双苯亚甲基环己酮(2a~2e)和2,5-双苯亚甲基环戊酮(5a);2a~2e或5a分别与硫脲或尿素经Biginelli反应合成了8个新型的姜黄素类似物(3a~3e,4a,4c和6a),其结构经1H NMR,13C NMR,IR和MS表征。利用DPPH法比较3~6与姜黄素的抗氧化能力。实验结果表明:3~6的抗氧化能力均比姜黄素母核结构高;3比4和6的自由基清除能力强;随用药量增大,抗氧化能力呈现先增强后下降的趋势,并在0.09 mg·mL-1~0.12 mg·mL-1自由基清除率达最大。 相似文献
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A novel efficient synthetic route to 1,3-dihydrobenzo[c]furan glycone was developed and the corresponding 5-fluoro, 5-iodo uracil and guanosine derivatives, the aromatic analogues of the well known antiviral 2',3'-dideoxy-2',3'-dihydronucleosides (d4N), were synthesized. 相似文献
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Florian M. Kruse Jennifer S. Teichert Prof. Dr. Oliver Trapp 《Chemistry (Weinheim an der Bergstrasse, Germany)》2020,26(65):14776-14790
Ever since the discovery of nucleic acids 150 years ago,[1] major achievements have been made in understanding and decrypting the fascinating scientific questions of the genetic code.[2] However, the most fundamental question about the origin and the evolution of the genetic code remains a mystery. How did nature manage to build up such intriguingly complex molecules able to encode structure and function from simple building blocks? What conditions were required? How could the precursors survive the unhostile environment of early Earth? Over the past decades, promising synthetic concepts were proposed providing clarity in the field of prebiotic nucleic acid research. In this Minireview, we show the current status and various approaches to answer these fascinating questions. 相似文献
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Triazolo-fused 3',4'-cyclic nucleoside 4'-spiro nucleoside analogues were synthesized by an intramolecular 1,3-dipolar cycloaddition of 4'-azido nucleoside derived azido-alkynes in a regio- and stereo-specific manner. The thymine nucleoside base in these target compounds was transformed into the corresponding 5-methyl cytosine component. The synthesized compounds were examined in an MAGI(multinuclear-activation galactosidase indicator) assay for exploring the anti-HIV activity and in a H9 T(human T lymphocytes H9) assay for measuring the cell toxicity. 相似文献
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Vasiliki Daikopoulou Panagiotis Apostolou Sofia Mourati Ioanna Vlachou Maria Gougousi Ioannis Papasotiriou 《Molecules (Basel, Switzerland)》2021,26(11)
Despite the fact that COVID-19 vaccines are already available on the market, there have not been any effective FDA-approved drugs to treat this disease. There are several already known drugs that through drug repositioning have shown an inhibitory activity against SARS-CoV-2 RNA-dependent RNA polymerase. These drugs are included in the family of nucleoside analogues. In our efforts, we synthesized a group of new nucleoside analogues, which are modified at the sugar moiety that is replaced by a quinazoline entity. Different nucleobase derivatives are used in order to increase the inhibition. Five new nucleoside analogues were evaluated with in vitro assays for targeting polymerase of SARS-CoV-2. 相似文献