组合化学-新药创制的高效方法与技术

整理文档很辛苦,赏杯茶钱您下走!

免费阅读已结束,点击下载阅读编辑剩下 ...

阅读已结束,您可以下载文档离线阅读编辑

资源描述

20034Apr.2003264JournalofChongqingUniversityVol.26No.4:1000-582X(2003)04-0080-06:X,,,(,400044):,,:,,,,:;;;;;:R914;O69;TQ655:A(Combichem)R.B.Merrifield[1](1984)1963,,,,60,Merrifield[1],,80,Geysen[2],Houghton[3]1991,[4]1996,Coronado,,CA1994120,12002000,[4-6],,,,,,,3:,,,,21,,,1,,,:,,,5,,(leadcom2pound),,,X:2002-12-03:[98][99-38][01-03-06]:(1977-),,,,,,,,,,-,200000,,,,,,,,,,,2,10,,?,n1+n2n1n2n1=n2=nnm,(SPOS):1);2);3);4);5);6)Chiron[6-8]SPOS,,[7-9],,SPOS,Ostresh,StepetovSR1,R2,,Rn,nP1,P2,,Pn,,,,,,SAR,,,,,,,,[10-14],,,,,3;;,,8,[14]Chiron(Peptoid),N-,,,Mannich18264::Ugi,MN3,2,,:1);2),;3),;4)(DNA),[15-17]4,,,,(),(),(),,,,MitsunobuUgi,,5,,,:,(TLC),,,,,,,(IR),FTIRFTIR(DRIFTS),,,NMR,NMR19F13C,,,31PNMR,31PNMRHornerWadsworthEmmons[17]NMR,,1HMR[18][17-20](MS),,,3MS:MS(MALDI2TOFMS),MS(TOF2SIMS)MS(ESI2MS)MALDI2TOFMSRinkN-,[21-22];TOF2SIMS,[23];ESI2MSCE171[24]6,[24-26],:1);2)(MCR)3CR282003,,,()[24-26],,,,PPP,,8%10%CAC-2000[24-25]1997-2002[26-29]:1);2);3);4);5);6);7);8);9);10)8,1)5)8)10),:1);2)();3),,,,;4),,,:,,;,,,[26-29],,,,(5%),7,,,,,(),,,,,Pfizer31000,AbbottHIV()(),,(VL),VL,VL,,(GA)(NN),,,KickVLD,WeberVLGA,Ugi,AbbottVL,FK-506(FKB)[30][31]Xiang,,,,,[32],,[32-33]82038264::,,,,,,,,,,:1);2);3);4)21,,,,,,,:[1]MERRIFIELDRB.SolidPhasePeptideSynthesis.I:TheSyn2thesisofaTetrapeptide[J].JAmChemSoc,1963,85:2149-2154.[2]GEYSENHM,MELOENRH,BARTELINGSJ.UseofPep2tideSynthesistoProbeViralAntigensforEpitopestoaResolu2tionofaSingleAminoAcid[J].ProcNatlAcadSciUSA,1984,81:3998-3999.[3]HOUGHTENRA.GeneralMethodfortheRapidSolidPhaseSyn2thesisofLargeNumbersofPeptides:SpecificityofAntigenAntibodyInteractionatthelevelofIndividualAminoAcids[J].ProcNatlAcadSciUSA,1985,82:5131-5136.[4]GALLOPMA,BARRETTRW,DOWERWJ,etal.Applica2tionofCombinatorialTechnologiestoDrugDiscovery1:Back2groundandPeptideCombinatorialLibraries[J].JMedChem,1994,37(9):1233-1251.[5]THOMPSONLA,ELLMANJA.SynthesisandApplicationsofSmallMoleculeLibraries[J].ChemRev,1996,96(1):555-600.[6]GEYSENHM,RODDASJ,MASONTJ.APriorDelineationofaPeptidewhichMimicsaDiscontinuousAntigenicDetermi2nant[J].MolImmunol,1986,23:709-715.[7]HOUGHTENRA,PINILLAC,BLONDELLESE,etal.TheUseofSyntheticPeptideCombinatorialLibrariesfortheIdentifi2cationofBioactivePeptides[J].Nature,1991,354:84-87.[8]FREIERSM,KONINGSDAM,WYATTJR,etal.Deconvolu2tionofCombinatorialLibrariesforDrugDiscover[J].JMedChem,1995,38:344-352.[9]JEFFREYJM.MeasuringDiversity:ExperimentalDesignofCombinatorialLibrariesforDrugDiscovery[J].JMedChem,1995,38:1431-1436.[10]CHEMINATA,BENEZRAC,FARRALLMJ,etal.Affinity2capillaryElectrophoresis2massSpectrometryforScreeningCom2binatorialLibraries[J].TetrahedronLett,1980,21:617-618.[11]CHANTY,CHENR,SOFIAMJ,etal.HighThroughputOn2beadMonitoringofSolidPhaseReactionsbyDiffuseReflec2tanceInfraredFourierTransformSpectroscopy(DRIFTS)[J].TetrahedronLett,1997,38:2821-2824.[12]GEYSENHM,WAGNERCD,BODNARWM,etal.Iso2topeorMassEncodingofCombinatorialLibraries[J].ChemBiol,1996,3:679-688.[13]XIAOXY,ZHAOC,POTASHH,etal.CombinatorialChem2istrywithLaserOpticalEncoding[J].AngewChemIntEdEn2gl,1997,36:780-782.[14]TERRETTNK,BOJANICD,BROWND,etal.TheCombi2natorialSynthesisofa30,7522compoundLibrary:DiscoveryofSARAroundtheEndothelinAntagonist,FR2139,317[J].BioorgMedChemLett,1995,5:917-922.[15]JOHNSONCR,ZHANGB.Solid2phaseSynthesisofAlkenesUsingtheHorner2Wadsworth2EmmonsReactionandMonitoringbyGel2phase31PNMR[J].TetrahedronLett,1995,36:9253-9256.[16]FITCHWL,DETREG,HOLMESCP.High2Resolution1HNMRinSolid2PhaseOrganicSynthesis[J].JOrgChem,1994,59:7955-7956.[17]KIEFERPA.InfluenceofResinStructure,TetherLength,andSolventupontheHigh2resolutionHNMRSpectraofSolid2phase2synthesisResins[J].JOrgChem,1996,61:1558-1589.[18]CHUYH,DUNAYEVSKIYYM,KIRBYDP,etal.Affinity2capillaryElectrophoresis2massSpectrometryforScreeningCom2binatorialLibraries[J].JAmChemSoc,1995,118:7827-7835.[19]YANB,KUMARAVELG,ANJARIAH,etal.InfraredSpectrumofaSingleResinBeadforReal2timeMonitoringofSolid2phasere2actions[J].JOrgChem,1995,60:5736-5738.[20]EGNERBJ,CARDNOM,BRADLEYM.LinkersforCombi2natorialChemistryandReactionAnalysisUsingSolidPhaseinSituMassSpectrometry[J].JChemSocChemCommun,1995,21:2163-2164.[21]BRUMMELCL,LEEINW,ZHOUY,etal,AMassSpectro2metricSolutiontotheAddressProblemofCombinatorialLibrar2ies[J].Science,1994,264:399-402.[22]WANGGT,LIS,WIDEBURGN,etal.SyntheticChemicalDiversitySolidPhase:SynthesisofLibrariesofC2SymmetricInhibitorsofHIVProteaseContainingDiaminoDiolandDiami2noAlcoholCores[J].JMedChem,1995,38:2995-3002.[23]ROBRERSP,BIRZINET,MOSLEYRT,etal.Rapid482003IdentificationofSubtype2selectiveAgonistsoftheSomatostatinReceptorthroughCombinatorialChemistry[J].Science,1998,282:737-740.[24]KEVINB.CombinatorialTechnologiesInvolvingReiterativeDi2visionPCouplingPRecombination:StatisticalConsiderations[J].JMedChem,1996,37:2985-2987.[25].[D].:,2002.[26],S,,.Diels2Alder[J].,1997,42(20):2175-2178.[27],Y,,.[J].,1997,5(2):123-132.[28]LIAOC,HOUM,LIB,etal.Applicationofchemometricsingreenchemistry1:ApproachesandApplicationsofChemomet2ricsinCombinatorialChemistry2:MultivariateStatistics,LatentRegressio

1 / 6
下载文档,编辑使用

©2015-2020 m.777doc.com 三七文档.

备案号:鲁ICP备2024069028号-1 客服联系 QQ:2149211541

×
保存成功