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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 FarmacijaSraka, Tina, farmacevtkaEncim 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, seriousPublication and manufacture - Ljubljana : [T. Sraka], 2022Language - slovenianCOBISS.SI-ID - 103409411
Author
Sraka, Tina, farmacevtka
Other authors
Gobec, Stanislav, 1970- |
Košak, Urban
Topics
Alzheimerjeva bolezen |
butirilholin-esteraza |
zaviralci butirilholin-esteraze |
N-benzilpiperidini |
sintetizirane spojine |
sinteza sulfonamidov
Library/institution |
City | Acronym | For loan | Other holdings |
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Faculty of Pharmacy, Ljubljana | Ljubljana | FFALJ |
reading room 1 cop.
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Sraka, Tina, farmacevtka | |
Gobec, Stanislav, 1970- | 15284 |
Košak, Urban | 33908 |
Source: Personal bibliographies
and: SICRIS
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