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Načrtovanje, sinteza in vrednotenje novih N-benzilpiperidinov kot zaviralcev holin-esteraz = Design, synthesis and evaluation of novel N-benzylpiperidines as cholinesterase inhibitors : enoviti magistrski študijski program Farmacija
Sraka, Tina, farmacevtka
Encim butirilholin-esteraza (BChE) postaja vse bolj pomembna tarča za lajšanje simptomov Alzheimerjeve bolezni. S selektivnim zaviranjem BChE lahko pomembno zvišamo koncentracijo acetilholina v ...možganih in tako vplivamo na potek bolezni. Na podlagi kemijske strukture spojine 2, ki je prvi nekovalentni selektivni zaviralec BChE s farmakološkim delovanjem in vivo, smo načrtovali in sintetizirali deset novih spojin z namenom poglobitve razumevanja odnosa med kemijsko strukturo in biološko učinkovitostjo. Sledilo je in vitro določanje jakosti zaviranja s pomočjo Ellmanove metode. Osem od desetih sintetiziranih spojin je bilo in vitro aktivnih, najmočnejši zaviralec BChE pa je bila spojina 10 (IC50 = 0,21 μM). V magistrski nalogi smo tako ugotovili, da je naftalen ključen za močnejše zaviranje BChE in obenem poglobili znanje o odnosu med strukturo in delovanjem selektivnih zaviralcev BChE.
Type of material - master's thesis
; adult, serious
Publication and manufacture - Ljubljana : [T. Sraka], 2022
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