Copper(I)-catalyzed　terminal　alkyne-azide　1,3-cycloaddition　reaction　has　emerged　as　one　of　the　main　strategies　for　the　rapid　creation　and　screening　of　a　small　molecular　library.　The　present　work　describes　the　design　and　synthesis　of　a　series　of　1,2,3-triazol-4-yl-substituted　1,4-dihydro-4-oxo-1,5-napthyridine-3-carboxylic　acids　in　which　the　hydrophobic　and　hydrophilic　domains　were　efficiently　incorporated　by　a　click　reaction.　The　Structures　of　the　desired　products　8　and　12　were　characterized　by　spectroscopic　methods　and　their　HIV　integrase　inhibitory　activities　were　also　screened.