Synthesis of an Anti-AIDs Drug Delavirdine Derivate, Resdelasu

(整期优先)网络出版时间:2008-06-16
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Inviewoftheanti-HIVactivitiesofdelavirdineandresveratrol,anovelanti-AIDsdrugResdelasu,1-{3-[(1-methyl-ethyl)amino]-2-pyridinyl}-4-{[5-(4-{5[(1E)-2-(hydroxyphenyl)ethenyl]-1,3-benzenedioyl-carbonylbu-tanoyl}amino)-1H-indol-2-yl]carbonyl}-piperazinewassynthesizedbylinkingthedelavirdinederivativeandresveratrolwithsuccinicanhydrideastheconjugatedcompoundviatwodifferentroutes.Itsstructurewasconfirmedbymeansof1HNMR,13CNMR,IR,MS,andelementalanalysis.TherouteofesterificationfollowedbyamidationforsynthesizingResdelasuwassimplerandgaveahigheryield(46%)thanthatofamidationfollowedbyesterification.ItwasprovedthatthemethodwasefficientandconvenienttoprepareResdelasu.TheresultsofHIV-1ReverseTranscriptaseAssayandquantitativetitrationofHIV-1viaMAGIassayshowedthatanovelanti-AIDsdrug,Resdelasu,hadbeensynthesized.