title: Technetium labeling of bi, tri and tetradentate ligands derived from 2-aminocyclopentene-1-dithiocarboxylic acid: characterization and biodistribution of their oxo and nitrido 99mtechnetium complexes.
abstract: We have synthesized and characterized seven ligands derived from 2-aminocyclopentene-1-dithiocarboxylic acid with different donor sets (SN2-, SNO2-, SNN2-, SNNO3- and SNNN3-) and different substituents on the sulfur moieties-SR (with R = H, CH3 or C2H5O(CH3)CH). With five of these ligands technetium nitrido complexes have been obtained with high yields (over 95%) using rather harsh conditions (pH = 1, temperature > or = 80 degrees C), whereas for technetium oxo complexes similar high yields were only obtained with two ligands but with mild conditions (pH = 7-8, temperature approximately equal to 50 degrees C). Changing an OH group for an NH2 has a drastic effect upon labeling yields. The possibility of complexing ligands as either oxo (TcO)3+ or nitrido (TcN)2+ derivatives increases the number of available labeled agents with different overall change and consequently with different biological behavior.
authors.affiliation: Laboratoire D'imagerie Morphologique et Fonctionnelle, Faculté de Medecine Toulouse-Purpan, France.
authors.forename: H
authors.initials: H
authors.lastname: Belhadj-Tahar
authors.forename: Y
authors.initials: Y
authors.lastname: Coulais
authors.forename: G
authors.initials: G
authors.lastname: Cros
authors.forename: M H
authors.initials: MH
authors.lastname: Darbieu
authors.forename: J A
authors.initials: JA
authors.lastname: Tafani
authors.forename: J
authors.initials: J
authors.lastname: Fabre
authors.forename: J P
authors.initials: JP
authors.lastname: Esquerré
authors.forename: R
authors.initials: R
authors.lastname: Guiraud
mesh_terms: D000818:Animals; D007553:Isotope Labeling / Q000379:methods; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D013329:Structure-Activity Relationship; D013667:Technetium / Q000493:pharmacokinetics; D013871:Thiones / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D014961:X-Ray Diffraction
chemical_list: D008024:Ligands; D013871:Thiones; D013667:Technetium