Abstract
In this work, 10 new asymmetrical tetradentate SNNO ligands were prepared by reaction of the amine function of methyl 2-[(beta-aminoethyl)amino]cyclopentene-1-dithiocarboxylate with various bifunctional substituents bearing hydroxyl/ketone and hydroxyl/aldehyde functional groups and with diethyl oxalate. 99mTc labeling efficiency was optimized by adjusting temperature and pH conditions. Seven nitrido and two oxo 99mTc complexes were isolated. Six of them proved to be stable near physiological conditions. Biodistribution studies in the rat showed a significant heart uptake for four of them and strong kidney and liver uptake for the other two.
MeSH terms
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Animals
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Cyclopentanes / chemical synthesis*
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Cyclopentanes / chemistry
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Cyclopentanes / pharmacokinetics*
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Drug Stability
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Ethylenediamines / chemical synthesis*
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Ethylenediamines / pharmacokinetics*
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Hydrogen-Ion Concentration
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Isotope Labeling
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Ligands
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Male
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacokinetics*
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Rats
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Rats, Wistar
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Technetium Compounds / chemical synthesis*
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Technetium Compounds / pharmacokinetics*
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Temperature
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Thiones / chemical synthesis*
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Thiones / chemistry
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Thiones / pharmacokinetics*
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Tissue Distribution
Substances
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Cyclopentanes
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Ethylenediamines
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Ligands
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Radiopharmaceuticals
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Technetium Compounds
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Thiones
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methyl-2-aminocyclopentene-1-dithiocarboxylic acid