Synthesis, labelling and biological characteristics of derivatives of Mercaptoacetyltriglycine with two amide functions
| Autor: | Paul Adriaens, S. M. Okarvi, Kristin Verbeke, Alfons Verbruggen |
|---|---|
| Rok vydání: | 2002 |
| Předmět: |
chemistry.chemical_classification
medicine.drug_class Stereochemistry Organic Chemistry Carboxamide Peptide Tripeptide Biochemistry Chemical synthesis Analytical Chemistry chemistry.chemical_compound chemistry Diagnostic agent Labelling Amide Drug Discovery medicine Radiology Nuclear Medicine and imaging Spectroscopy Biological evaluation |
| Zdroj: | Journal of Labelled Compounds and Radiopharmaceuticals. 45:115-137 |
| ISSN: | 1099-1344 0362-4803 |
| DOI: | 10.1002/jlcr.538 |
| Popis: | Eight novel derivatives of MAG3, containing in their structure two instead of three amide functions, have been synthesized and evaluated. The synthesized ligands were labelled with 99mTc by exchange labelling at 100°C and/or by a direct labelling method at room temperature. After labelling with 99mTc, the reaction mixtures were analyzed by radio-HPLC. Biological evaluation of different 99mTc-diamide complexes in mice and a baboon indicated that substitution in one amide function of MAG3 structure greatly influences the renal handling of these compounds. It was found that the diamide derivatives containing at least one inverted amide exhibit biological behavior comparable to that of 99mTc-MAG3. Copyright © 2002 John Wiley & Sons, Ltd. |
| Databáze: | OpenAIRE |
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