Synthesis of Two 3,5-Disubstituted Sulfonamide Catechol Ligands and Evaluation of Their Iron(III) Complexes for Use as MRI Contrast Agents

Two 3,5-disubstituted sulfonamide catechol ligands were synthesized. Tris(ligand) iron(III) complexes were prepared and investigated as MRI contrast agents. Longitudinal relaxivity (r1) values were determined for the complexes. The r1 values in water were substantially higher than those of typical s...

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Veröffentlicht in:Journal of medicinal chemistry 2005-11, Vol.48 (23), p.7482-7485
Hauptverfasser: Schwert, Daniel D, Richardson, Nicholas, Ji, Gongjun, Radüchel, Bernd, Ebert, Wolfgang, Heffner, Peter E, Keck, Rick, Davies, Julian A
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Sprache:eng
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Zusammenfassung:Two 3,5-disubstituted sulfonamide catechol ligands were synthesized. Tris(ligand) iron(III) complexes were prepared and investigated as MRI contrast agents. Longitudinal relaxivity (r1) values were determined for the complexes. The r1 values in water were substantially higher than those of typical six-coordinate iron(III) complexes. The r1 values in plasma under the same conditions increased. The iron(III) complexes were administered to rats, and the kidney and liver signal intensities were measured by T1-weighted MR imaging experiments.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm0501984