Role of Protecting Groups in the Preparation of Thiolate Complexes of Technetium-99m using Cysteine as a Mode

Roy, U and Chatterjee Debnath, M and Sanyal, Kasturi and Das, M K and Banerjee, S (2006) Role of Protecting Groups in the Preparation of Thiolate Complexes of Technetium-99m using Cysteine as a Mode. JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, 49 (10). pp. 835-847.

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    Abstract

    An attempt has been made to develop a suitable protecting group for the thiolate function for 99mTc binding ligands having such function and which could be deprotected automatically during 99mTc-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 99mTc–l-cysteine, the authentic standard chelate, by HPLC. The corresponding 99Tc chelate of cysteine from l-cystine and S-thiomethyl l- cysteine was also prepared. It was found that the 99Tc chelates exhibited similar retention profiles to those of the corresponding 99mTc chelates in reverse phase HPLC. The results of the biodistribution studies after 99mTc chelation were likewise compared to those of 99mTc-l-cysteine. The effect of probenecid on renal excretion was studied only on the 99mTc 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

    Item Type: Article
    URI: http://www.eprints.iicb.res.in/id/eprint/499
    Subjects: Structural Biology & Bioinformatics
    Divisions: Indian Institute of Chemical Biology
    Depositing User: Mr Shyamal Nath
    Date Deposited: 02 Nov 2011 15:52
    Last Modified: 03 Feb 2012 14:30
    Official URL: htpp://dx.doi.org/10.1002/jlcr.1084
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