About: Synthesis of new (arylcarbonyloxy)aminopropanol derivatives and the determination of their physico-chemical properties

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
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. (en)
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 (en)
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 (en)
skos:notation	RIV/62157124:16370/13:43872136!RIV14-MSM-16370___
http://linked.open...avai/predkladatel	Farmaceutická fakulta
http://linked.open...avai/riv/aktivita	I P S
http://linked.open...avai/riv/aktivity	I, P(ED1.1.00/02.0073), S
http://linked.open...iv/cisloPeriodika	11
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Kapustíková, Iva Mokrý, Petr Csöllei, Jozef Tengler, Jan Jampílek, Josef
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Veterinární a farmaceutická univerzita Brno / Farmaceutická fakulta
http://linked.open...dnocenehoVysledku	109539
http://linked.open...ai/riv/idVysledku	RIV/62157124:16370/13:43872136
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Ultrashort effect; H-1 NMR spectroscopy; Acid dissociation constant; Beta-blockers; Aryloxyaminopropanol (en)
http://linked.open.../riv/klicoveSlovo	Beta-blockers Acid dissociation constant Aryloxyaminopropanol Ultrashort effect H-1 NMR spectroscopy
http://linked.open...odStatuVydavatele	PL - Polská republika
http://linked.open...ontrolniKodProRIV	[3B543423393A]
http://linked.open...i/riv/nazevZdroje	Central European Journal of Chemistry
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	5 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...vavai/riv/projekt	CzechGlobe - Center for Global Climate Change Impacts Studies
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	11
http://linked.open...iv/tvurceVysledku	Csöllei, Jozef Jampílek, Josef Mokrý, Petr Oravec, Michal Tengler, Jan Kapustíková, Iva Stropnický, Ondřej
http://linked.open...ain/vavai/riv/wos	000324816000006
issn	1895-1066
number of pages	11 (xsd:int)
http://bibframe.org/vocab/doi	10.2478/s11532-013-0302-8
http://localhost/t...ganizacniJednotka	16370

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