Diketo　acid　derivatives　are　potent　and　selective　HIV-1　integrase　inhibitors.　To　investigate　the　detailed　synthesis　of　those　derivatives,　a　series　of　p/m-[p-(un)substituted　phenylsulfonamidolphenyl　beta-diketo　acid　derivatives　have　been　designed　and　synthesized.　The　quinoxalone　derivatives　as　the　potential　bioisosteres　of　the　biologically　labile　beta-diketoacid　pharmacophores　have　also　been　synthesized　from　reactions　of　the　corresponding　diketo　acids　with　o-phenylenediamine.　The　structures　of　all　diketo　acid　(ester)　and　quinoxalone　derivatives　were　confirmed　by　H-1　NMR,　C-13　NMR,　IR,　HRMS　and/or　MS　(ESI).　X-ray　crystallographic　analysis　of　11b　demonstrates　a　similar　arrangement　of　the　side　chain　of　quinoxalone　derivatives　with　the　parent　diketoacids　due　to　the　intramolecular　hydrogen　bond　(O　center　dot　center　dot　center　dot　H-N)　and　the　sp(2)　hybridization　configuration　of　the　two　nitrogen　atoms　of　the　quinoxalone　ring.