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 

机构地区：[1]School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P R. China

出　　处：《Chemical Research in Chinese Universities》2010年第2期225-229,共5页高等学校化学研究（英文版）

基　　金：Supported by the National Natural Science Foundation of China(No.20872082);the Natural Science Foundation of Shandong Province,China(No.Y2007C060)

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 ^1H 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.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 ^1H 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.

关 键 词：HIV-1 integrase Diketoacid FURANONE 

分 类 号：TQ460.72[医药卫生—药物分析学] O626.11[化学工程—制药化工]