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
通讯作者地址：[Zhao, GS]Shandong Univ, Sch Pharmaceut Sci, Jinan 250012, Peoples R China.
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.