Role of protecting groups in the preparation of thiolate complexes of technetium-99m using cysteine as a model
Metadata of CSIR Papers
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Title |
Role of protecting groups in the preparation of thiolate complexes of technetium-99m using cysteine as a model
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Creator |
Roy, U
Debnath, MC Sanyal, K Das, MK Banerjee, S |
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Subject |
Biochemical Research Methods; Chemistry, Medicinal; Chemistry, Analytical; Pharmacology & Pharmacy
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Description |
An attempt has been made to develop a suitable protecting group for the thiolate function for Tc-99m binding ligands having such function and which could be deprotected automatically during Tc-99m-chelation without the use of any additional reagents. As a model ligand a simple molecule like L-cysteine was selected. Seven S-protected derivatives of this amino acid were synthesized, radiolabelled with technetium-99m under a variety of experimental conditions and the yield of the desired chelate was compared to that of Tc-99m-L-cysteine, the authentic standard chelate, by HPLC. The corresponding Tc-99 chelate of cysteine from L-cystine and S-thiomethyl L-cysteine was also prepared. It was found that the Tc-99 chelates exhibited similar retention profiles to those of the corresponding Tc-99m chelates in reverse phase HPLC. The results of the biodistribution studies after Tc-99m chelation were likewise compared to those of Tc-99m-L-cysteine. The effect of probenecid on renal excretion was studied only on the Tc-99m chelate of S-thiomethyl-L-cysteine to determine whether tubular excretion was involved. The results suggest that the S-thiomethyl group could be used as an ideal protective group to mask the high reactivity of thiolate functions attached to different Tc-99m binding ligands. Copyright (c) 2006 John Wiley & Sons, Ltd.
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Publisher |
JOHN WILEY & SONS LTDCHICHESTERTHE ATRIUM, SOUTHERN GATE, CHICHESTER PO19 8SQ, W SUSSEX, ENGLAND
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Date |
2011-09-20T12:12:06Z
2011-09-20T12:12:06Z 2006 |
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Type |
Article
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Identifier |
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
0362-4803 http://hdl.handle.net/123456789/14123 |
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Language |
English
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