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Statements

Subject Item
n2:RIV%2F60077344%3A_____%2F07%3A00094858%21RIV08-AV0-60077344
rdf:type
skos:Concept n8:Vysledek
dcterms:description
In positron emission tomography (PET) alpha-methyl amino acids have two potential applications: As analogues of neutransmitter precursors for the study of neurodegenerative diseases, and as non-metabolised analogues of proteinogenic amino acids for the study of amino acid uptake into normal and cancer cells. Clinical applications of such amino acids are strongly limited due to their poor availability. We carried out [C-11]methylation of metalocomplex synthons derived from protected DOPA or tyrosine. After 10min at 25 ºC, a 9% radiochemical yield (decay-corrected) of a mixture of the diastereomeric alpha-[C-11]methylDOPA complexes or a 7% radiochemical yield of a mixture of the diastereomeric alpha-[C-11]methyltyrosine complexes was achieved. Optimisation of the procedure including hydrolysis of the complexes (hydrolytic deprotection of enantiomerically pure amino acids) and subsequent purification of the enantiomers of a-[11C]methyID0PA and alpha-[C-11]methyltyrosine is underway. V pozitronové emisní tomografii (PET) alfa-amino kyseliny mají dvě aplikace: jako analogy neurotransmiterových prekurzorů při studiu neurodegenerativních onemocnění a jako nemetabolizované analogy proteinotvorných aminokyselin při studiu rakovinových buněk. Klinické aplikace modifikovaných aminokyselin jsou omezeny jejich nedostupností. V prácie zkoumána [C-11] methylace metalokomplexních synthonů DOPA a tyrosinu. Při 25ºC po 10 min. byly získány s 9% výtěžkem diastereomerní komplexy směsi alfa-[C-11] methylDOPA a se 7% výtěžkem směs alpha-[C-11]methyltyrosinového komplexu. Optimalizace postupu včetně hydrolýzy komplexů a čištění enantiomerů alfa-[11C]methyID0PA and alfa-[C-11]methyltyrosinu jsou ve vývoji. In positron emission tomography (PET) alpha-methyl amino acids have two potential applications: As analogues of neutransmitter precursors for the study of neurodegenerative diseases, and as non-metabolised analogues of proteinogenic amino acids for the study of amino acid uptake into normal and cancer cells. Clinical applications of such amino acids are strongly limited due to their poor availability. We carried out [C-11]methylation of metalocomplex synthons derived from protected DOPA or tyrosine. After 10min at 25 ºC, a 9% radiochemical yield (decay-corrected) of a mixture of the diastereomeric alpha-[C-11]methylDOPA complexes or a 7% radiochemical yield of a mixture of the diastereomeric alpha-[C-11]methyltyrosine complexes was achieved. Optimisation of the procedure including hydrolysis of the complexes (hydrolytic deprotection of enantiomerically pure amino acids) and subsequent purification of the enantiomers of a-[11C]methyID0PA and alpha-[C-11]methyltyrosine is underway.
dcterms:title
Towards stereoselective radiosynthesis of alpha-[C-11]methylsubstituted aromatic alpha-amino acids - a challenge of creation of quaternary asymmetric centre in a very short time Towards stereoselective radiosynthesis of alpha-[C-11]methylsubstituted aromatic alpha-amino acids - a challenge of creation of quaternary asymmetric centre in a very short time Stereoselectivní radiosyntéza alfa-[C-11]methylsubstituovaných aromatických alfa-amino acids – stimul k syntéze kvarterního asymetrického centra ve velmi krátké době
skos:prefLabel
Stereoselectivní radiosyntéza alfa-[C-11]methylsubstituovaných aromatických alfa-amino acids – stimul k syntéze kvarterního asymetrického centra ve velmi krátké době Towards stereoselective radiosynthesis of alpha-[C-11]methylsubstituted aromatic alpha-amino acids - a challenge of creation of quaternary asymmetric centre in a very short time Towards stereoselective radiosynthesis of alpha-[C-11]methylsubstituted aromatic alpha-amino acids - a challenge of creation of quaternary asymmetric centre in a very short time
skos:notation
RIV/60077344:_____/07:00094858!RIV08-AV0-60077344
n4:strany
370;374
n4:aktivita
n12:S n12:Z
n4:aktivity
S, Z(AV0Z50070508), Z(MSM6007665808)
n4:cisloPeriodika
5-6
n4:dodaniDat
n14:2008
n4:domaciTvurceVysledku
n16:1267698
n4:druhVysledku
n11:J
n4:duvernostUdaju
n15:S
n4:entitaPredkladatele
n5:predkladatel
n4:idSjednocenehoVysledku
455408
n4:idVysledku
RIV/60077344:_____/07:00094858
n4:jazykVysledku
n17:eng
n4:klicovaSlova
asymmetric synthesis; alfa-methyl amino acids; carbon-11
n4:klicoveSlovo
n10:carbon-11 n10:alfa-methyl%20amino%20acids n10:asymmetric%20synthesis
n4:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n4:kontrolniKodProRIV
[5211640C6556]
n4:nazevZdroje
Journal of Labelled Compounds and Radiopharmaceuticals
n4:obor
n6:CE
n4:pocetDomacichTvurcuVysledku
1
n4:pocetTvurcuVysledku
6
n4:rokUplatneniVysledku
n14:2007
n4:svazekPeriodika
50
n4:tvurceVysledku
Kružberská, Pavla Nádvorník, M. Lyčka, A. Lehel, S. Popkov, A. Gillings, N.
n4:zamer
n13:AV0Z50070508 n13:MSM6007665808
s:issn
0362-4803
s:numberOfPages
5