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Eur J Med Chem ; 39(5): 467-72, 2004 May.
Article in English | MEDLINE | ID: mdl-15110973

ABSTRACT

A simple procedure was developed to compare chelating agents for (153)Sm complexes as a preliminary step to synthesise bifunctional analogues. Several variables affecting the efficiency of complex stability were investigated, such as the pre-organisation concept, cavity size, and the nature of coordination sites. Four semi-rigid agents incorporating carboxylic and/or phosphonic groupings fixed at trans-1,2-diaminocyclohexane were evaluated for their (153)Sm chelation properties, and competition studies were performed. Data on the stability of the best chelating agent compound 3: trans-cyclohexane-1,2-bis(aminomethylphosphonic)-N,N'-bis(ethyl-2-iminodiacetic acid) in human serum are presented.


Subject(s)
Carboxylic Acids/chemistry , Chelating Agents/chemistry , Cyclohexylamines/chemistry , Organometallic Compounds/chemistry , Organophosphonates/chemistry , Samarium/chemistry , Cyclohexylamines/chemical synthesis , Drug Stability , Humans , Isotope Labeling/methods , Ligands , Organometallic Compounds/blood , Organometallic Compounds/chemical synthesis , Organophosphorus Compounds/chemistry , Radioisotopes , Samarium/blood
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