A　series　of　novel　beta-diketo　derivatives　which　combined　the　virtues　of　dihydroxypyrimidine　carboxamide　derived　from　the　evolution　of　DKA　and　polyhydroxylated　aromatics　moieties,　were　designed　and　synthesized　as　potential　HIV-1　integrase　(IN)　inhibitors　and　evaluated　their　inhibition　to　the　strand　transfer　process　of　HIV-1　integrase　and　anti-HIV-1　activity.　The　result　indicates　that　3,4,5-trihydroxylated　aromatic　derivatives　exhibit　good　inhibition　to　HIV-1　integrase,　but　dihydroxylated　aromatic　derivatives　appear　little　inhibition　to　HIV-1　integrase.　In　addition,　the　preliminary　structure-activity　relationship　(SAR)　of　these　new　derivatives　was　rationalized　by　docking　studies.　(c)　2014　Elsevier　Ltd.　All　rights　reserved.