抗艾滋病药物Delavirdine衍生物Resdelasu的合成

IF 3.1 4区 化学 Q2 CHEMISTRY, MULTIDISCIPLINARY
Qing-xiang GUAN , Li-peng HE , Xi WANG , Wen-yan ZHANG , En-si WANG , Xiang-hui YU
{"title":"抗艾滋病药物Delavirdine衍生物Resdelasu的合成","authors":"Qing-xiang GUAN ,&nbsp;Li-peng HE ,&nbsp;Xi WANG ,&nbsp;Wen-yan ZHANG ,&nbsp;En-si WANG ,&nbsp;Xiang-hui YU","doi":"10.1016/S1005-9040(09)60016-7","DOIUrl":null,"url":null,"abstract":"<div><p>In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[(1-methyl-ethyl)amino]-2-pyridinyl}-4-{[5-(4-{5[(1<em>E</em>)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino)-1<em>H</em>-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound <em>via</em> two different routes. Its structure was confirmed by means of <sup>1</sup>H NMR, <sup>13</sup>C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield(46%) than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 <em>via</em> MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized.</p></div>","PeriodicalId":9785,"journal":{"name":"Chemical Research in Chinese Universities","volume":"24 6","pages":"Pages 731-734"},"PeriodicalIF":3.1000,"publicationDate":"2008-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/S1005-9040(09)60016-7","citationCount":"0","resultStr":"{\"title\":\"Synthesis of an Anti-AIDs Drug Delavirdine Derivate, Resdelasu\",\"authors\":\"Qing-xiang GUAN ,&nbsp;Li-peng HE ,&nbsp;Xi WANG ,&nbsp;Wen-yan ZHANG ,&nbsp;En-si WANG ,&nbsp;Xiang-hui YU\",\"doi\":\"10.1016/S1005-9040(09)60016-7\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[(1-methyl-ethyl)amino]-2-pyridinyl}-4-{[5-(4-{5[(1<em>E</em>)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino)-1<em>H</em>-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound <em>via</em> two different routes. Its structure was confirmed by means of <sup>1</sup>H NMR, <sup>13</sup>C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield(46%) than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 <em>via</em> MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized.</p></div>\",\"PeriodicalId\":9785,\"journal\":{\"name\":\"Chemical Research in Chinese Universities\",\"volume\":\"24 6\",\"pages\":\"Pages 731-734\"},\"PeriodicalIF\":3.1000,\"publicationDate\":\"2008-11-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/S1005-9040(09)60016-7\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Chemical Research in Chinese Universities\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1005904009600167\",\"RegionNum\":4,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Chemical Research in Chinese Universities","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1005904009600167","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0

摘要

鉴于德拉韦林和白藜芦醇的抗hiv活性,将德拉韦林衍生物和白藜芦醇以琥珀酸酐为偶联物,经两种不同途径连接,合成了一种新型抗艾滋病药物瑞德拉苏,1-{3-[(1-甲基-乙基)氨基]-2-吡啶基}-4-{[5-(4-{5[(1E)-2-(羟基苯基)乙烯基]-1,3-苯二酰基羰基丁基}氨基)-1 -吲哚-2-羰基}-哌嗪。通过1H NMR、13C NMR、IR、MS和元素分析证实了其结构。采用酯化-酰胺化法合成redelasu比酰胺化-酯化法更简单,产率(46%)更高。结果表明,该方法简便、高效。HIV-1逆转录酶测定和MAGI定量测定HIV-1的结果表明,合成了一种新的抗艾滋病药物redelasu。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Synthesis of an Anti-AIDs Drug Delavirdine Derivate, Resdelasu

In view of the anti-HIV activities of delavirdine and resveratrol, a novel anti-AIDs drug Resdelasu, 1-{3-[(1-methyl-ethyl)amino]-2-pyridinyl}-4-{[5-(4-{5[(1E)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonylbutanoyl}amino)-1H-indol-2-yl]carbonyl}-piperazine was synthesized by linking the delavirdine derivative and resveratrol with succinic anhydride as the conjugated compound via two different routes. Its structure was confirmed by means of 1H NMR, 13C NMR, IR, MS, and elemental analysis. The route of esterification followed by amidation for synthesizing Resdelasu was simpler and gave a higher yield(46%) than that of amidation followed by esterification. It was proved that the method was efficient and convenient to prepare Resdelasu. The results of HIV-1 Reverse Transcriptase Assay and quantitative titration of HIV-1 via MAGI assay showed that a novel anti-AIDs drug, Resdelasu, had been synthesized.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
CiteScore
5.30
自引率
6.50%
发文量
152
审稿时长
3.0 months
期刊介绍: The journal publishes research articles, letters/communications and reviews written by faculty members, researchers and postgraduates in universities, colleges and research institutes all over China and overseas. It reports the latest and most creative results of important fundamental research in all aspects of chemistry and of developments with significant consequences across subdisciplines. Main research areas include (but are not limited to): Organic chemistry (synthesis, characterization, and application); Inorganic chemistry (bio-inorganic chemistry, inorganic material chemistry); Analytical chemistry (especially chemometrics and the application of instrumental analysis and spectroscopy); Physical chemistry (mechanisms, catalysis, thermodynamics and dynamics); Polymer chemistry and polymer physics (mechanisms, material, catalysis, thermodynamics and dynamics); Quantum chemistry (quantum mechanical theory, quantum partition function, quantum statistical mechanics); Biochemistry; Biochemical engineering; Medicinal chemistry; Nanoscience (nanochemistry, nanomaterials).
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信