A　series　of　novel　beta-diketo　derivatives　which　combined　the　virtues　of　1,3-diketo,　1,2,3-triazole　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.　The　result　indicates　that　3,4,5-trihydroxylated　aromatic　derivatives　exhibit　good　inhibition　to　HIV-1　integrase,　but　dihydroxylated　aromatic　derivatives　and　corresponding　methoxy　aromatic　derivatives　appear　little　inhibition　to　HIV-1　integrase.　(C)　2011　Elsevier　Ltd.　All　rights　reserved.