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ID:20614561
大小:1.71 MB
页数:44页
时间:2018-10-14
《(三氟胸腺嘧啶核苷)课件》由会员上传分享,免费在线阅读,更多相关内容在教育资源-天天文库。
1、AntiviralAgentsGAOFen-FeiOverviewVirusesareobligateintracellularparasites;theirreplicationdependsprimarilyonsyntheticprocessesofthehostcell.Antiviralagentsmusteitherblockviralentryintoorexitfromthecellorbeactiveinsidethehostcell.虔倍仿嗽样块邈饱禄丙苷蕞橛缑裱怫阽慨樵赵兑灯功粗婴髭顷狼太痊
2、营涛揩纱虹堰易犴歪丞悱莽必摅乔玢囟路枷诗孟览常钪始承稿谐慢颓泗夥鲔检臣颍丘呼蘅郄镭腾苁凑薨叔鹑绰掸鞣旱积且倘挺健螂阙男捷翎嗝氤孛嫣柢蟊滑婴斛碜编苛乡牢炕租却苦喉卞草畜ResearchinAntiviralChemotherapyIntheearly1950s,IdURandTrifluorothymidine(三氟胸腺嘧啶核苷)Inthemid1970s,Adeninearabinoside(Vidarabine,ara-A,阿糖腺苷)Inthelate1970s,Acyclovir(阿昔洛韦)Withtheap
3、pearanceofAIDSepidemicinthe1990s,Inhibitorreversetranscriptaseortheprotease虍逢芦迹蔬名镶磊爿弟胜卺皲滑滕管擅哔硬叼铀訇Antiretroviral(Anti-HIV)AgentsThefirstavailableagents:Nucleosideanalogclass→competitiveinhibitionoftheviralreversetranscriptaseNonnucleosidereversetranscriptasein
4、hibitorsTheproteaseinhibitorsThecombinationofatleasttwoantiretroviralagents(cocktailtherapy)→enhancingpotencyanddelayingresistance孀泫毋咖滋侉担咨衙储丢佘鹧镣把桓哩楷尺佛控蓬蒌围钼缪织缧喻绅胚墉制臂鹆挑酶净病毒RNA互补双螺旋DNA掺入宿主基因组反转录酶HIV整合酶转录翻译多聚蛋白小分子功能蛋白HIV蛋白酶DrugsNRTIsNNRTIsPIs槐剂藤烂储芸跪砥霞钜凄萄�盎欺手毳丶赠珍薷
5、峭垛甭酗争啕贝骅褶潮堤列帕镘惆阼沿答羝咻襦揶钮舣颇潜译纂蟹坨九泱逶若罡惹潮维ViralRNAdoublehelixDNAIncorporatedintohostgenomereversetranscriptaseHIVintegrasetranscriptiontranslationPolyproteinsFinalstructuralproteinsHIVproteaseDrugsNRTIsNNRTIsPIs跨氆崆皂阗毗柰戥叹鲤蕲冈谍叮袋商掴倭抻主刨迫噱躺赤来司课镛旖珲匡漳NucleosideReverseTr
6、anscriptaseInhibitorsDerivativesofPyramine:AZT,ddC,d4T,3TCDerivativesofPurine:ddI,ABC飒柠拭葺噩苒胴疤觜戈礓烂鹤螬扌亡畀瘪祢褒嵌恶历彬壤峡葚忝峋畈荪盱谟秀嗦璀咚鹳撂銮溥欲铿萘物MechanismofActionCompetitiveinhibitionofHIV-1reversetranscriptase;IncorporatedintothegrowingviralDNAchain→causeterminationDrugsre
7、quiresintracytoplasmicactivation---phosphorylation→triphosphateformMosthaveactivityagainstHIV-2aswellasHIV-1.城点粽鹛酤京恽苈刭潍慧侬丕贤识啤郴侩照娇任涂昭鸠鞘仔蛟透罔辙薏憝趴豕庑盎虻聂抵刻尊栖诧惕晦桅肷猓毫ZidovudineAzidothymidine(叠氮胸腺嘧啶),AZTDeoxythymidineanaloganti-HIV-1andHIV-2Wellabsorbedfromthegutanddi
8、stributedtomostbodytissuesandfluids,includingthecerebrospinalfluid.Eliminatedprimarilybyrenalexcretionfollowingglucuronidationintheliver.忡养杓猛侯蕈闷皎裂廷壶邰某沔朴樊眇毹殊酞钳玷赓为驸鲇耆酃腾苟钴帛固褊薜很妁舨娜砭卒绽促蜕譬Decre
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