Production of Meta-Iodobenzilguanidine, 123I Preparation for Medical Diagnostics

2015 ◽  
Vol 1084 ◽  
pp. 451-455
Author(s):  
Ilyas E. Slamkulov ◽  
Viktor S. Skuridin ◽  
Aleksey S. Semenov ◽  
Aleksandr A. Garapatsky
Keyword(s):  
Ammonium Sulfate ◽  
Radiochemical Purity ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Medical Diagnostics ◽  
Phase Synthesis ◽  
Experimental Animals ◽  
Experimental Installation ◽  
Iodine 123

This paper demonstrates a method for production of the radiopharmaceutical meta-iodobenzilguanidin (MIBG) labeled with radionuclide iodine-123 (123I). An experimental installation has been developed and the conditions of solid-phase synthesis of the preparation have been described. The influence of the content of ammonium sulfate in the reaction mixture and the temperature and duration of dry synthesis on the process of labeling has been researched. It has been established experimentally that when the ratio of MIBG and ammonium sulfate is 1:4, it is efficient to carry out synthesis at the temperature of 150°C to rapidly obtain a preparation with radiochemical purity of over 97%. Biomedical tests of the synthesized preparation have been carried out in experimental animals. Its functional suitability for scintigraphic studies has been shown.

Synthesis and Screening of A DNA-Encoded Library of Non-Peptidic Macrocycles

2020 ◽  
Author(s):  
Eric Koesema ◽  
Animesh Roy ◽  
Nicholas G. Paciaroni ◽  
Thomas Kodadek
Keyword(s):  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Cell Permeability ◽  
Phase Synthesis ◽  
Protein Ligands ◽  
High Affinity ◽  
Scaffold Diversity

There is considerable interest in the development of libraries of non-peptidic macrocycles as a source of ligands for difficult targets. We report here the solid-phase synthesis of a DNA-encoded library of several hundred thousand thioether-linked macrocycles. The library was designed to be highly diverse with respect to backbone scaffold diversity and to minimize the number of amide N-H bonds, which compromise cell permeability. The utility of the library as a source of protein ligands is demonstrated through the isolation of compounds that bind streptavidin, a model target, with high affinity.

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