|
OALib Journal期刊
ISSN: 2333-9721
费用：99美元
|
|
|
|
新型乙酰胆碱酯酶抑制剂的设计、合成与活性研究
, PP. 346-351
Keywords: 2-氨基-4-苯基噻唑,乙酰胆碱酯酶抑制剂,阿尔茨海默病
Abstract:
本文设计、合成了一类全新结构类型的2-氨基-4-苯基噻唑类化合物，并考察了这些化合物对乙酰胆碱酯酶活性的抑制作用。以α-溴代苯乙酮为起始原料，经hantzsch、酰化和取代反应合成了2-氨基-4-苯基噻唑类化合物，并利用ellman分光光度法考察了它们对乙酰胆碱酯酶（ache）的体外抑制活性。实验结果表明目标化合物均具有一定的ache抑制活性，其中化合物8a抑制活性最好，其ic50达到了3.54μmol·l-1，优于对照药利斯的明。2-氨基-4-苯基噻唑类化合物对乙酰胆碱酯酶具有较好的抑制活性，需要进一步深入研究。
| [1] | zhangjt.pathogenesisandtherapeuticstrategiesofseniordementia[j].actapharmsin(药学学报),2000,35:635-640.
|
| [2] | cummingsjl.treatmentofalzheimer’sdisease:currentandfuturetherapeuticapproaches[j].revneuroldis,2004,1:60-69.
|
| [3] | rongxf,wangxl.anoverviewofbiomarkersinalzheimer’sdisease[j].actapharmsin(药学学报),2012,47:551-557.
|
| [4] | yangwc,sunq,yunx,etal.designofacetylcholinesteraseinhibitorforalzheimer’sdiseasetherapy:frommulti-bindingsiteinhibitorstomulti-targetdirectedligands[j].actapharmsin(药学学报),2012,47:313-321.
|
| [5] | matsumurak,onom,kimurah,etal.18f-labeledphenyldiazenylbenzothiazoleforinvivoimagingofneurofibrillarytanglesinalzheimer’sdiseasebrains[j].acsmedchemlett,2012,3:58-62.
|
| [6] | gómez-islat,hollisterr,westh,etal.neuronallosscorrelateswithbutexceedsneurofibrillarytanglesinalzheimer’sdisease[j].annneurol,1997,41:17-24.
|
| [7] | alzheimer’sassociation,thiesw,bleilerl.2011alzheimer’sdiseasefactsandfigures[j].alzheimersdement,2011,7:208-244.
|
| [8] | bartusrt,deanld3rd,beerb,etal.thecholinergichypothesisofgeriatricmemorydysfunction[j].science,1982,217:408-414.
|
| [9] | glennergg,wongcw.alzheimer’sdiseaseanddown’ssyndrome:sharingofauniquecerebrovascularamyloidfibrilprotein[j].biochembiophysrescommun,1984,122:1131-1135.
|
| [10] | glennergg,wongcw.alzheimer’sdisease:initialreportofthepurificationandcharacterizationofanovelcerebrovascularamyloidprotein[j].biochembiophysrescommun,1984,120:885-890.
|
| [11] | gauthiers,poirierj.currentandfuturemanagementofalzheimer’sdisease[j].alzheimersdement,2008,4:s48-s50.
|
| [12] | scarpinie,scheltensp,feldmanh.treatmentofalzheimer’sdisease:currentstatusandnewperspectives[j].lancetneurol,2003,2:539-547.
|
| [13] | arriagadapv,growdonjh,hedley-whyteet,etal.neurofibrillarytanglesbutnotsenileplaquesparalleldurationandseverityofalzheimer’sdisease[j].neurology,1992,42:631-639.
|
| [14] | gongrm.thelinearmixedinhibitionkineticsamongreverisibleinhibitiontoenzyme[j].janhuinormaluniv(natsci)(安徽师范大学学报(自然科学版)),1998,21:46-49.
|
| [15] | ellmangl,courtneykd,andresv,etal.anewandrapidcolorimetricdeterminationofacetylcholinesteraseactivity[j].biochempharmacol,1961,7:88-95.
|
Full-Text
|
|
Contact Us
service@oalib.com QQ:3279437679 
WhatsApp +8615387084133
|
|
