A　series　of　novel　6-(pyrazolylmethyl)-4-oxo-4H-quinoline-3-carboxylic　acid　derivatives　bearing　different　substituents　on　the　N-position　of　quinoline　ring　were　designed　and　synthesized　as　potential　HIV-1　integrase　(IN)　inhibitors,　based　on　the　structurally　related　GS-9137　scaffold.　The　structures　of　all　new　compounds　were　confirmed　by　H-1-NMR,　C-13-NMR　and　ESI　(or　HRMS)　spectra.　Detailed　synthetic　protocols　and　the　anti-IN　activity　studies　are　also　presented.