Detail
Článek
Článek online
FT
Medvik - BMČ
  • Je něco špatně v tomto záznamu ?

Low molecular weight precursor applicable for Alzheimer disease drugs synthesis (AChE and BChE inhibition, BACE inhibition, antioxidant properties and in silico modulation)

Lucie Drtinova, Petr Dobes, Miroslav Pohanka

. 2014 ; 12 (4) : 285-290.

Jazyk angličtina Země Česko

Typ dokumentu práce podpořená grantem, hodnotící studie

Perzistentní odkaz   https://www.medvik.cz/link/bmc15018294

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

Bibliografie atd.

Literatura

000      
00000naa a2200000 a 4500
001      
bmc15018294
003      
CZ-PrNML
005      
20151012172227.0
007      
ta
008      
150525s2014 xr f 000 0|eng||
009      
AR
024    7_
$2 doi $a 10.1016/j.jab.2014.01.010
040    __
$a ABA008 $d ABA008 $e AACR2 $b cze
041    0_
$a eng
044    __
$a xr
100    1_
$a Drtinová, Lucie $7 _AN029254 $u Faculty of Military Health Sciences, University of Defense, Hradec Kralove, Czech Republic
245    10
$a Low molecular weight precursor applicable for Alzheimer disease drugs synthesis (AChE and BChE inhibition, BACE inhibition, antioxidant properties and in silico modulation) / $c Lucie Drtinova, Petr Dobes, Miroslav Pohanka
504    __
$a Literatura
520    9_
$a 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
650    12
$a Alzheimerova nemoc $x farmakoterapie $7 D000544
650    _2
$a techniky in vitro $x statistika a číselné údaje $7 D066298
650    12
$a farmaceutická chemie $x metody $x statistika a číselné údaje $7 D002626
650    _2
$a neurodegenerativní nemoci $x farmakoterapie $7 D019636
650    _2
$a cholinesterasové inhibitory $x farmakologie $7 D002800
650    _2
$a sekretasy $x antagonisté a inhibitory $7 D053829
650    _2
$a aspartátové endopeptidasy $x antagonisté a inhibitory $7 D016282
650    _2
$a počítačová simulace $7 D003198
650    _2
$a tryptofan $x farmakologie $7 D014364
650    _2
$a pyridoxin $x farmakologie $7 D011736
650    _2
$a tryptaminy $x farmakologie $7 D014363
650    _2
$a akridiny $x farmakologie $7 D000166
650    _2
$a chinoliny $x farmakologie $7 D011804
650    _2
$a isochinoliny $x farmakologie $7 D007546
650    _2
$a indoly $x farmakologie $7 D007211
650    _2
$a pyridiny $x farmakologie $7 D011725
650    _2
$a piperidiny $x farmakologie $7 D010880
650    _2
$a antioxidancia $x farmakologie $7 D000975
655    _2
$a práce podpořená grantem $7 D013485
655    _2
$a hodnotící studie $7 D023362
700    1_
$a Dobeš, Petr $7 _AN051505 $u Masaryk Memorial Cancer Institute in Brno, Brno, Czech Republic
700    1_
$a Pohanka, Miroslav $7 hka2010563580 $u Faculty of Military Health Sciences, University of Defense, Hradec Kralove, Czech Republic; Karel English College in Brno, Brno, Czech Republic
773    0_
$t Journal of applied biomedicine $x 1214-021X $g Roč. 12, č. 4 (2014), s. 285-290 $w MED00012667
856    41
$u https://jab.zsf.jcu.cz/pdfs/jab/2014/04/13.pdf $y plný text volně přístupný
910    __
$a ABA008 $b B 2301 $c 1249 $y 4 $z 0
990    __
$a 20150522215938 $b ABA008
991    __
$a 20151012172416 $b ABA008
999    __
$a ok $b bmc $g 1078527 $s 901225
BAS    __
$a 3
BMC    __
$a 2014 $b 12 $c 4 $d 285-290 $i 1214-021X $m Journal of Applied Biomedicine $x MED00012667
LZP    __
$c NLK121 $d 20151012 $a NLK 2015-26/dk

Najít záznam

Citační ukazatele

Možnosti archivace