Faculty of Pharmacy, Lj. (FFALJ)
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Načrtovanje, sinteza in vrednotenje večfunkcionalnih ligandov z delovanjem na adrenergične receptorje in holin esteraze = Design, synthesis and evaluation of multifunctional ligands targeting adrenergic receptors and cholinesterases : enovit magistrski študijski program Farmacija : Uniform Master's Study Programme PharmacyGruden, StašAlzheimerjeva bolezen (AB) je večfunkcionalna nevrodegenerativna bolezen, kjer poleg upada holinergičnega prenosa pride tudi do motenj v delovanju noradrenergičnega sistema v možganih. Pri ... napredovani obliki AB se poveča aktivnost butirilholin esteraze (BChE), ki nadomesti acetilholin esterazo kot prevladujoča holin esteraza v holinergičnih sinapsah, večje aktivno mesto BChE pa omogoča racionalno načrtovanje selektivnih zaviralcev tega encima. Vezava oligomerov amiloida β na α2A adrenergične receptorje (α2AAR) aktivira kinazo GSK3β in vodi v hiperfosforilacijo proteina tau. Učinkovine, ki hkrati delujejo na oba nevrotransmitorska sistema, imajo večji potencial za učinkovitejše zdravljenje, ki bi lahko upočasnilo nevrodegenerativne procese v možganih. V magistrski nalogi smo načrtovali in sintetizirali 10 spojin, ki naj bi dosegle zaviranje človeške hBChE in delovale antagonistično na α2AAR. Izhodišče je predstavljal atipamezol (znan selektiven antagonist α2AR), na katerega smo z reakcijo N-aciliranja uvedli karbamatno skupino ključno za zaviranje holin esteraz. Zaviralno aktivnost zoper obe holin esterazi so izkazovali zgolj karbamati (7, 8, 11–13 in 16), ki so preko kovalentnega načina vezave zavirali hBChE. Vsi karbamati, razen spojine 11, so encim zavirali v nanomolarnih koncentracijah, izkazovali pa so tudi selektivnost napram acetilholin esterazi. Največji potencial za nadaljnjo optimizacijo ima spojina 16, ki selektivno zavira hBChE z IC50 vrednostjo 2,39 nM.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [S. Gruden], 2023Language - slovenianCOBISS.SI-ID - 151834627
Author
Gruden, Staš
Other authors
Knez, Damijan, farmacevt |
Meden, Anže
Topics
Alzheimerjeva bolezen |
Nevrodegenerativne bolezni |
Zdravljenje |
butirilholin esteraza |
adrenergični receptor α2A |
kovalentni zaviralci |
večfunkcionalne spojine
Call number – location, accession no. ... |
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Knjižnica emšf 0000000616 GRUDEN STAŠ Načrtovanje 0000001242 IN: 0017679 Knjižnica emšf 616 GRUDEN STAŠ Načrtovanje 1242 IN: 0017679 |
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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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Gruden, Staš | |
Knez, Damijan, farmacevt | 36438 |
Meden, Anže | 53584 |
Source: Personal bibliographies
and: SICRIS
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