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Statements

Subject Item
n2:RIV%2F60162694%3AG44__%2F14%3A43875216%21RIV15-MO0-G44_____
rdf:type
n7:Vysledek skos:Concept
rdfs:seeAlso
http://obd3.hk.pmfhk.cz/fcgi/verso.fpl/_TS_/1418907937/dload/3017550/Drtinova%20JAB%202014.pdf
dcterms:description
Alzheimer disease (AD) is the most common cause of progressive dementia in the elderly population, with prevalence of 5% after 65 year of age and is increasing to about 30% in people over 85 year. AD is a neurodegenerative and incurable disease. Currently, three inhibitors of acetylcholinesterase (AChE), galantamine, donepezil and rivastigmine, and one inhibitor of N-methyl-d-aspartate (NMDA) receptor are available as drugs for amelioration of the disease. Demand to prepare drugs for the therapy providing at least relieve of symptoms remains. In this experiment, the ability of standards (donepezil, galantamine, huperzine A, tacrine and 7-methoxytacrine) and precursors used for synthesis of new AD drugs (l-tryptophan, pyridoxine B6, tryptamine, acridine, chinoline, isochinoline, indole, pyridine and piperidine) to inhibit AChE, BChE and BACE or to have the antioxidant properties were determined. The results were compared using statistical expression of the relationship between the performed tests. In this experiment, IC50 for every one method and every compound were found. Beside this, prediction of free energy in a link to ln(IC50) was assessed using in silico tests. This article focuses on possibility to find the most suitable chemical precursors to be used in the next development of drugs for AD. Alzheimer disease (AD) is the most common cause of progressive dementia in the elderly population, with prevalence of 5% after 65 year of age and is increasing to about 30% in people over 85 year. AD is a neurodegenerative and incurable disease. Currently, three inhibitors of acetylcholinesterase (AChE), galantamine, donepezil and rivastigmine, and one inhibitor of N-methyl-d-aspartate (NMDA) receptor are available as drugs for amelioration of the disease. Demand to prepare drugs for the therapy providing at least relieve of symptoms remains. In this experiment, the ability of standards (donepezil, galantamine, huperzine A, tacrine and 7-methoxytacrine) and precursors used for synthesis of new AD drugs (l-tryptophan, pyridoxine B6, tryptamine, acridine, chinoline, isochinoline, indole, pyridine and piperidine) to inhibit AChE, BChE and BACE or to have the antioxidant properties were determined. The results were compared using statistical expression of the relationship between the performed tests. In this experiment, IC50 for every one method and every compound were found. Beside this, prediction of free energy in a link to ln(IC50) was assessed using in silico tests. This article focuses on possibility to find the most suitable chemical precursors to be used in the next development of drugs for AD.
dcterms:title
Low molecular weight precursor applicable for Alzheimer disease drugs synthesis (AChE and BChE inhibition, BACE inhibition, antioxidant properties and in silico modulation) Low molecular weight precursor applicable for Alzheimer disease drugs synthesis (AChE and BChE inhibition, BACE inhibition, antioxidant properties and in silico modulation)
skos:prefLabel
Low molecular weight precursor applicable for Alzheimer disease drugs synthesis (AChE and BChE inhibition, BACE inhibition, antioxidant properties and in silico modulation) Low molecular weight precursor applicable for Alzheimer disease drugs synthesis (AChE and BChE inhibition, BACE inhibition, antioxidant properties and in silico modulation)
skos:notation
RIV/60162694:G44__/14:43875216!RIV15-MO0-G44_____
n4:aktivita
n5:I n5:S n5:P
n4:aktivity
I, P(ED2.1.00/03.0101), S
n4:cisloPeriodika
4
n4:dodaniDat
n10:2015
n4:domaciTvurceVysledku
n16:3876284 n16:7153082
n4:druhVysledku
n19:J
n4:duvernostUdaju
n18:S
n4:entitaPredkladatele
n20:predkladatel
n4:idSjednocenehoVysledku
26679
n4:idVysledku
RIV/60162694:G44__/14:43875216
n4:jazykVysledku
n9:eng
n4:klicovaSlova
Neurodegeneration; Betasecretase; Inhibition; Alzheimer disease; Acetylcholinesterase
n4:klicoveSlovo
n13:Acetylcholinesterase n13:Betasecretase n13:Alzheimer%20disease n13:Inhibition n13:Neurodegeneration
n4:kodStatuVydavatele
CZ - Česká republika
n4:kontrolniKodProRIV
[FA819AFE9691]
n4:nazevZdroje
Journal of Applied Biomedicine - print
n4:obor
n15:FR
n4:pocetDomacichTvurcuVysledku
2
n4:pocetTvurcuVysledku
3
n4:projekt
n6:ED2.1.00%2F03.0101
n4:rokUplatneniVysledku
n10:2014
n4:svazekPeriodika
12
n4:tvurceVysledku
Pohanka, Miroslav Drtinová, Lucie Dobeš, Petr
n4:wos
000345065200013
s:issn
1214-021X
s:numberOfPages
6
n8:doi
10.1016/j.jab.2014.01.010
n12:organizacniJednotka
G44