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001-es BibID:	BIBFORM010517
Első szerző:	Gama, Sofia
Cím:	Combined chelation of bi-functional bis-hydroxypiridinone and mono-hydroxypiridinone : Synthesis, solution and in vivo evaluation / Sofia Gamaa, Marco Gil, Lurdes Gano, Etelka Farkas, M. Amélia Santos
Dátum:	2009
ISSN:	0162-0134
Megjegyzések:	3-Hydroxy-4-pyridinones (3,4-HP) are well known iron-chelators with applications in medicinal chemistry, mainly associated with their high affinity towards trivalent hard metal ions (e.g. M3+ M = Fe, Al, Ga) and use as decorporating agents in situations of metal accumulation. The polydenticity and the extra-functionality of 3,4-HP derivatives have been explored, aimed at improving the chelating efficacy and the selectivity of the interaction with specific biological receptors. However, the ideal conjugation of both features in one molecular unity usually leads to high molecular weight compounds which can have crossing-membrane limitations. Herein, a different approach is used combining a arylpiperazine-containing bis-hydroxypyridone (H2L1) with a biomimetic mono-hydroxypyridinone, ornithine-derivative (HL2), to assess the potential coadjuvating effect that could result from the administration of both compounds for the decorporation of hard metal ions. This work reports the results of solution and in vivo studies on their chelating efficacy either as a simple binary or a ternary system (H2L1:HL2:M3+), using potentiometric and spectrophotometric methods. The solution complexation studies with Fe(III) indicate that the solubility of the complexes is considerably increased in the ternary system, an important feature for the metal complex excretion, upon the metal sequestration. The results of the in vivo studies With Ga-67-injected mice show differences on the biodistribution profiles of the radiotracer, upon the administration of each chelating agent, that are mainly ascribed to the differences of their extra-functional groups and lipo/hydrophilic character. However, administration of both chelating agents leads to a more steady metal mobilization, which may be attributed to an improved access to different cellular compartments. (C) 2008 Elsevier Inc. All rights reserved.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:	Journal Of Inorganic Biochemistry. - 103 : 2 (2009), p. 288-298. -
További szerzők:	Gil, Marco Gano, Lurdes Farkas Etelka (1948-) (vegyész) Santos, Amélia M.
Internet cím:	DOI Intézményi repozitóriumban (DEA) tárolt változat
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001-es BibID:	BIBFORM084834
Első szerző:	Santos, Amélia M.
Cím:	A new bis(3-hydroxy-4-pyridinone)-IDA derivative as a potential therapeutic chelating agent : synthesis, metal-complexation and biological assays / M. Amélia Santos, Sofia Gama, Lurdes Gano, Guilhermina Cantinho, Etelka Farkas
Dátum:	2004
ISSN:	1477-9226
Megjegyzések:	A new bis(3-hydroxy-4-pyridinone) derivative of iminodiacetic acid, imino-bis(acetyl(1-(3'-aminopropyl)-3-hydroxy-2-methyl-4-pyridinone)), IDAPr(3,4-HP)(2), has been prepared and studied in its interaction with a set of hard metal ions. This tetradentate ligand presents a much higher chelating efficiency for trivalent hard metal ions (Fe, Ga, Al) than the monodentate derivative Deferriprone, namely at the diluted conditions prevailing in physiological conditions and at low clinical doses. A similar behaviour was also observed for the complexation with Zn(II) but at a significantly lower extent. This compound presents a moderate hydrophilic character at physiological pH (logD=-1.72). In vivo assays showed much more rapid clearance of (67)Ga from most tissues of metal-loaded mice than the drug Deferriprone and the radioactivity excretion occurs mostly through the kidneys. Therefore, results from in vitro and in vivo studies indicated good perspectives for this compound to be a potential decorporating agent for hard metal ions in overload situations without depletion of essential metal ions such as zinc.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Dalton Transactions. - 2004 : 21 (2004), p. 3772-3781. -
További szerzők:	Gama, Sofia Gano, Lurdes Cantinho, Guilhermina Farkas Etelka (1948-) (vegyész)
Pályázati támogatás:	OTKA T034674 OTKA
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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001-es BibID:	BIBFORM082443
Első szerző:	Santos, Amélia M.
Cím:	Bis(3-hydroxy-4-pyridinone)-EDTA derivative as a potential therapeutic Al-chelating agent : synthesis, solution studies and biological assays / M. Amélia Santos, Sofia Gama, Lurdes Gano, Etelka Farkas
Dátum:	2005
ISSN:	0162-0134
Megjegyzések:	The 3-hydroxy-4-pyridinones are chelating agents of current interest due to their high affinity for hard metal ions and potential clinical applications as metal-decorporation agents. A new bis-(3-hydroxy-4-pyridinone) derivative of EDTA have been developed, and herein we describe the results of solution studies to determine the protonation constants and the partition coefficient. Biodistribution studies, performed with 67Ga-overload mice, showed rapid clearance of the radiotracer from the body, thus indicating that the new ligand should be a quite effective agent for the in vivo aluminium removal.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Journal of Inorganic Biochemistry. - 99 : 9 (2005), p. 1845-1852. -
További szerzők:	Gama, Sofia Gano, Lurdes Farkas Etelka (1948-) (vegyész)
Pályázati támogatás:	OTKA T049612 OTKA
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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