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Vpliv zamenjave aromatskega obroča v indolinskih zaviralcih butirilholin esteraze in z mitogenom aktivirane kinaze p38α = Influence of aromatic replacement in indoline inhibitors of butyrylcholinesterase and mitogen-activated protein kinase p38α : magistrska naloga : magistrski študij industrijska farmacijaBevk, Ana, farmacevtkaMagistrska naloga obravnava novejši pristop k zdravljenju Alzheimerjeve bolezni (AB) z načrtovanjem in sintezo novih dvojnih zaviralcev, ki so usmerjeni proti dvema ključnima encimoma butirilholin ... esterazi (BChE) in z mitogenom aktivirani kinazi p38α (p38α MAPK). Alzheimerjeva bolezen je nevrodegenerativna motnja, za katero je značilen upad kognitivnih sposobnosti in je tesno povezana z disregulacijo holinergične nevrotransmisije in nevrovnetnih procesov, ki jih posreduje p38α MAPK. Zaviranje BChE izboljša kognitivne funkcije zaradi povečanja koncentracije živčnega prenašalca acetilholina, zaviranje kinaze p38α MAPK pa zmanjša nevrovnetje in hiperfosforilacijo proteina tau, kar bi lahko izboljšalo klinične znake, ki se kažejo pri AB. Na osnovi selektivnega zaviralca p38 MAPK, spojine ARRY-371797, smo načrtovali in sintetizirali pet novih spojin, označenih s številkami 9, 10, 16, 22 in 28 v šeststopenjski sintezi, pri čemer smo izhajali iz metil 2-fluoro-4-metil-5-nitrobenzoata. Naše končne spojine se razlikujejo od spojine ARRY-371797 v aromatskih substituentih, ki zamenjajo 2,4-difluorofenilno skupino v spojini vodnici. Z novimi substituenti smo želeli ohraniti ali povečati jakost zaviranja p38α MAPK in BChE. Spojine smo očistili, potrdili njihovo strukturo s spektroskopskimi metodami in jim izmerili aktivnost s pomočjo biokemijskih testiranj na rekombinantnih encimih. Izmed vseh zaviralcev se je za najobetavnejšega izkazala spojina 9, ki zavira človeško (h)BChE z IC50 vrednostjo 6,4 µM in p38α MAPK z IC50 = 0,28 µM.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [A. Bevk], 2024Language - slovenianCOBISS.SI-ID - 188289283
Author
Bevk, Ana, farmacevtka
Other authors
Obreza, Aleš |
Košak, Urban
Topics
Nevrodegenerativne bolezni |
Alzheimerjeva bolezen |
BChE |
p38α MAPK |
načrtovanje dvojnih zaviralcev |
sintezni postopki
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Library | Call number – location, accession no. ... | Copy status |
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Faculty of Pharmacy, Lj. | Knjižnica mind 616 BEVK ANA Vpliv 308 IN: 0018095 |
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Bevk, Ana, farmacevtka | ![]() |
Obreza, Aleš | 19061 |
Košak, Urban | 33908 |
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