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Titolo:
TRIETHYLENETETRAMINE-N,N,N'N''N'''N'''-HEXAACETIC ACID (TTHA) AND TTHA-BIS(BUTANAMIDE) AS CHELATING-AGENTS RELEVANT TO RADIOPHARMACEUTICAL APPLICATIONS
Autore:
ACHOUR B; COSTA J; DELGADO R; GARRIGUES E; GERALDES CFGC; KORBER N; NEPVEU F; PRATA MI;
Indirizzi:
UNIVERSITE PAUL SABATIER,LAB SYNTH PHYSICOCHIM & RADIOBIOL F-31062 TOULOUSE 4 FRANCE UNIVERSITE PAUL SABATIER,LAB SYNTH PHYSICOCHIM & RADIOBIOL F-31062 TOULOUSE 4 FRANCE INST TECNOL QUIM & BIOL P-2780 OEIRAS PORTUGAL FAC FARM P-1600 LISBON PORTUGAL INST SUPER TECN,DEQ P-1096 LISBON PORTUGAL UNIV COIMBRA,DEPT BIOQUIM P-3000 COIMBRA PORTUGAL UNIV COIMBRA,CTR NEUROCIENCIAS P-3000 COIMBRA PORTUGAL UNIV BONN D-6000 FRANKFURT GERMANY
Titolo Testata:
Inorganic chemistry
fascicolo: 11, volume: 37, anno: 1998,
pagine: 2729 - 2740
SICI:
0020-1669(1998)37:11<2729:TA(AT>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
NUCLEAR-MAGNETIC-RESONANCE; LOW-DENSITY LIPOPROTEINS; AQUEOUS-SOLUTION; STABILITY-CONSTANTS; TRIETHYLENETETRAAMINEHEXAACETIC ACID; TUMOR-LOCALIZATION; COMPLEXES; COORDINATION; ALUMINUM; NMR;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
61
Recensione:
Indirizzi per estratti:
Citazione:
B. Achour et al., "TRIETHYLENETETRAMINE-N,N,N'N''N'''N'''-HEXAACETIC ACID (TTHA) AND TTHA-BIS(BUTANAMIDE) AS CHELATING-AGENTS RELEVANT TO RADIOPHARMACEUTICAL APPLICATIONS", Inorganic chemistry, 37(11), 1998, pp. 2729-2740

Abstract

The N,N'-bis(butanamide) derivative of TTHA (TTHA = triethylenetetramine-N,N,N',N'', N''', N'''- hexaacetic acid), and its Ga3+ and In3+ complexes were synthesized and characterized. The crystal X-ray diffraction structure of [Ga-2(OH)(2)(TTHA)] [Na-2(H2O)(6)] . 2H(2)O was determined. The complex crystallizes in the monoclinic space group P2(1)/n with a = 7.179(2) Angstrom, b = 20.334(3) Angstrom, c = 10.902(5) Angstrom, beta = 101.90(2)degrees, and Z = 2. Each gallium atom is bonded to six donor atoms (N2O4) in a slightly distorted octahedral geometry. The values of the protonation constants and the protonation sequence were determined by potentiometry and NMR. The stability constants of the Al3+, Ga3+, Fe3+, and In3+ complexes of TTHA-(BuA)(2) and of the Ga3+ complex of TTHA were determined by potentiometry. The structures, in solution, of the Al3+, Ga3+, and In3+ complexes of TTHA-(BuA)(2) andTTHA were analyzed by H-1, C-13, Al-27, Ga-71, and In-115 NMR techniques. Derivatization of two terminal carboxylates by butanamide substituents leads to a significant decrease of the total ligand basicity (5.77 log units) and to a change of the solubility of the resulting complexes. The stability constant of the ML complexes of TTHA-(BuA)(2) withFe3+ exhibits the highest value of the series (10(23.92)). The In3+ complex is more stable than that of Ga3+ and almost as stable as that of the Fe3+. However, the decrease in indium and iron complex stabilityis less drastic going from TTHA to TTHA-(BuA)(2) (about 3 log units) than for Al3+ or Ga3+ (about 6 log units). pM values calculated under physiological conditions for DTPA, TTHA, and the bis(butanamide) derivatives have shown that while DTPA remains a ligand of choice to chelate Fe3+ and In3+ ions in vivo compared to transferrin as competitor ligand, TTHA, surprisingly, appears to be the best of these four ligands (pM = 22.71) to chelate Ga3+.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 24/11/20 alle ore 14:40:30