Twenty novel furanone derivatives,based on the structure of raltegravir which was the first HIV-1 integrase(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.
YU Sheng-hui ZHAO Si-tai LIU Chuan ZHONG Yuan ZHAO Gui-sen
