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Synthesis, labelling and biological characteristics of derivatives of Mercaptoacetyltriglycine with two amide functions
Author(s) -
Okarvi S. M.,
Verbeke K.,
Adriaens P.,
Verbruggen A. M.
Publication year - 2002
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.538
Subject(s) - labelling , chemistry , amide , baboon , stereochemistry , combinatorial chemistry , organic chemistry , biochemistry , medicine
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 100°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 © 2002 John Wiley & Sons, Ltd.