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Statements

Subject Item
n2:RIV%2F62157124%3A16370%2F13%3A43872136%21RIV14-MSM-16370___
rdf:type
n5:Vysledek skos:Concept
dcterms:description
Eight hydrochlorides of 3-{2-[(2/4-flurophenoxy)-ethylamino]}-2-hydroxypropyl-4-alkoxybenzoates and four hydrochlorides of 3-tert-butylamino-2-hydroxypropyl-4-butoxybenzoates were prepared as potential antagonists of the beta 1-adrenergic receptor (beta-blockers). A multistep synthesis of these compounds is described as well as their detailed analytical characterization. The pharmacokinetic properties of these weak base compounds are significantly influenced by their acid-base dissociation constant, pK(a). The knowledge of this value is crucial for new drug development. This paper is aimed at developing a methodology that utilizes pH-dependent H-1 NMR spectroscopy for its routine analysis. The selected predicted physico-chemical parameters of the new (arylcarbonyloxy)aminopropanols (i.e., aryloxyaminopropanol derivatives) were compared with the model drugs esmolol and flestolol. Eight hydrochlorides of 3-{2-[(2/4-flurophenoxy)-ethylamino]}-2-hydroxypropyl-4-alkoxybenzoates and four hydrochlorides of 3-tert-butylamino-2-hydroxypropyl-4-butoxybenzoates were prepared as potential antagonists of the beta 1-adrenergic receptor (beta-blockers). A multistep synthesis of these compounds is described as well as their detailed analytical characterization. The pharmacokinetic properties of these weak base compounds are significantly influenced by their acid-base dissociation constant, pK(a). The knowledge of this value is crucial for new drug development. This paper is aimed at developing a methodology that utilizes pH-dependent H-1 NMR spectroscopy for its routine analysis. The selected predicted physico-chemical parameters of the new (arylcarbonyloxy)aminopropanols (i.e., aryloxyaminopropanol derivatives) were compared with the model drugs esmolol and flestolol.
dcterms:title
Synthesis of new (arylcarbonyloxy)aminopropanol derivatives and the determination of their physico-chemical properties Synthesis of new (arylcarbonyloxy)aminopropanol derivatives and the determination of their physico-chemical properties
skos:prefLabel
Synthesis of new (arylcarbonyloxy)aminopropanol derivatives and the determination of their physico-chemical properties Synthesis of new (arylcarbonyloxy)aminopropanol derivatives and the determination of their physico-chemical properties
skos:notation
RIV/62157124:16370/13:43872136!RIV14-MSM-16370___
n5:predkladatel
n6:orjk%3A16370
n3:aktivita
n18:I n18:S n18:P
n3:aktivity
I, P(ED1.1.00/02.0073), S
n3:cisloPeriodika
11
n3:dodaniDat
n15:2014
n3:domaciTvurceVysledku
n4:3170446 n4:7985479 n4:8728968 n4:9033793 n4:5909996
n3:druhVysledku
n20:J
n3:duvernostUdaju
n9:S
n3:entitaPredkladatele
n19:predkladatel
n3:idSjednocenehoVysledku
109539
n3:idVysledku
RIV/62157124:16370/13:43872136
n3:jazykVysledku
n14:eng
n3:klicovaSlova
Ultrashort effect; H-1 NMR spectroscopy; Acid dissociation constant; Beta-blockers; Aryloxyaminopropanol
n3:klicoveSlovo
n8:H-1%20NMR%20spectroscopy n8:Acid%20dissociation%20constant n8:Aryloxyaminopropanol n8:Ultrashort%20effect n8:Beta-blockers
n3:kodStatuVydavatele
PL - Polská republika
n3:kontrolniKodProRIV
[3B543423393A]
n3:nazevZdroje
Central European Journal of Chemistry
n3:obor
n17:FR
n3:pocetDomacichTvurcuVysledku
5
n3:pocetTvurcuVysledku
7
n3:projekt
n13:ED1.1.00%2F02.0073
n3:rokUplatneniVysledku
n15:2013
n3:svazekPeriodika
11
n3:tvurceVysledku
Stropnický, Ondřej Kapustíková, Iva Tengler, Jan Mokrý, Petr Csöllei, Jozef Oravec, Michal Jampílek, Josef
n3:wos
000324816000006
s:issn
1895-1066
s:numberOfPages
11
n12:doi
10.2478/s11532-013-0302-8
n11:organizacniJednotka
16370