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Synthesis, labelling and biological characteristics of derivatives of Mercaptoacetyltriglycine with two amide functions

✍ Scribed by S. M. Okarvi; K. Verbeke; P. Adriaens; A. M. Verbruggen


Publisher
John Wiley and Sons
Year
2002
Tongue
French
Weight
188 KB
Volume
45
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

Eight novel derivatives of MAG~3~, containing in their structure two instead of three amide functions, have been synthesized and evaluated. The synthesized ligands were labelled with ^99m^Tc by exchange labelling at 100Β°C and/or by a direct labelling method at room temperature. After labelling with ^99m^Tc, the reaction mixtures were analyzed by radio‐HPLC. Biological evaluation of different ^99m^Tc‐diamide complexes in mice and a baboon indicated that substitution in one amide function of MAG~3~ 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 ^99m^Tc‐MAG~3~. Copyright Β© 2002 John Wiley & Sons, Ltd.


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