标题:Synthesis and HIV-1 Integrase Inhibitory Activity of Furanone Derivatives
作者:Yu Sheng-hui; Zhao Si-tai; Liu Chuan; Zhong Yuan; Zhao Gui-sen
作者机构:[Yu, S.-H] School of Pharmaceutical Sciences, Shandong University, Jinan 250012, China;[ Zhao, S.-T] School of Pharmaceutical Sciences, Shandong Unive 更多
通讯作者:Zhao, GS(guisenzhao@sdu.edu.cn)
通讯作者地址:[Zhao, GS]Shandong Univ, Sch Pharmaceut Sci, Jinan 250012, Peoples R China.
来源:高等学校化学研究(英文版)
出版年:2010
卷:26
期:2
页码:225-229
关键词:HIV-1 integrase;Diketoacid;Furanone
摘要:Twenty novel furanone derivatives,based on the structure of raltegravir which was the first HIV-1 inte-grase(IN) inhibitor approved by the United States Food and Drug Administration(US FDA),were designed,synthesized and characterized by ]H NMR,IR and MS.The biological activities of these compounds against HIV-1 IN in vitro were evaluated.The assay results indicate that the replacement of pyrimidinone with furanone decreased the inhibitory activity of the compounds to HIV-1 IN.Compounds 3i,3j and 3t show moderate inhibitory activity against HIV-1 IN and selectively inhibit the strand transfer reaction.
收录类别:CSCD;SCOPUS;SCIE
WOS核心被引频次:1
Scopus被引频次:2
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-80052532608&partnerID=40&md5=e95c2f1d1b1b71561c41f350087f7df7
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