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Načrtovanje, sinteza in vrednotenje N-alkilpirolidin karbamatov kot zaviralcev holin esteraz in monoamin oksidaz = Design, synthesis and evaluation of N-alkylpyrrolidine carbamates as inhibitors of cholinesterases and monoamine oxidases : Uniform Master's Study Programm PharmcyMastnak-Sokolov, PeterNabor odobrenih zdravil za (simptomatsko) zdravljenje Alzheimerjeve bolezni (AB) in njihova učinkovitost sta razmeroma omejena, zato je potreba po razvoju novih učinkovin za terapijo te ... nevrodegenerativne bolezni izredno velika. Na tem področju so zelo zanimive molekule z delovanjem na več različnih tarč, udeleženih v kompleksni patofiziologiji AB. Dve izmed tarč potencialnih novih učinkovin za (simptomatsko) zdravljenje AB sta encima butirilholin esteraza (BChE) in monoamin oksidaza B (MAO-B) – izražanje obeh je v možganih bolnikov z AB povečano. Zaviranje BChE upočasni razgradnjo živčnega prenašalca acetilholina (ACh) in ublaži simptome AB brez holinergičnih neželenih učinkov, značilnih za zaviralce acetilholin esteraze (AChE). Zaviranje MAO-B zmanjša oksidativni stres, ki pospešuje nevrodegenerativne procese. Načrtovali in sintetizirali smo 30 novih N-alkilpirolidin karbamatov ter z encimskimi testi ovrednotili njihovo sposobnost zaviranja holin esteraz (ChE) in monoamin oksidaz (MAO) in vitro. Vse spojine z delovanjem na ChE so izkazale dobro selektivnost za zaviranje BChE v primerjavi z AChE. Najučinkovitejši zaviralci BChE iz serije [45 (IC50 = 22,24 nM), 46 (IC50 = 34,43 nM), 47 (IC50 = 27,16 nM) in 48 (IC50 = 21,02 nM)] so ta encim zavirale časovno odvisno, kar nakazuje na kovalentni mehanizem delovanja. Za spojino 45 smo kovalentni mehanizem zaviranja BChE potrdili z vrednotenjem encimske kinetike. Kovalentni mehanizem zaviranja najučinkovitejšega zaviralca MAO-B, spojine 36 (IC50 = 0,36 μM), je bil zaradi njene N-propargilne aminske skupine pričakovan. Med spojinami, ki zavirajo oba tarčna encima hkrati, je najbolj obetavna spojina 38 [IC50(BChE) = 34,69 μM; IC50(MAO-B) = 1,53 μM)]. S pričujočo magistrsko nalogo smo potrdili, da so N-alkilpirolidin karbamati zelo zanimivi novi zaviralci BChE oziroma MAO-B v nanomolarnem območju z velikim potencialom za razvoj v učinkovitejše in varnejše učinkovine za lajšanje simptomov in zdravljenje AB.Type of material - master's thesis ; adult, seriousPublication and manufacture - Ljubljana : [P. Mastnak-Sokolov], 2023Language - slovenianCOBISS.SI-ID - 156303875
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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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Mastnak-Sokolov, Peter | ![]() |
Gobec, Stanislav, 1970- | 15284 |
Košak, Urban | 33908 |
Source: Personal bibliographies
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