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 , Li-peng HE , Xi WANG , Wen-yan ZHANG , En-si WANG , 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 , Li-peng HE , Xi WANG , Wen-yan ZHANG , En-si WANG , 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}
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.
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).