Copyright (c) 2024 Barakat Shabsoug, Ned Heindel
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A Useful Method for in situ Indirect Radiolabeling of Carbonyl-Containing Biomolecules
Corresponding Author(s) : Barakat M. Shabsoug
Asian Journal of Chemistry,
Vol. 36 No. 3 (2024): Vol 36 Issue 3, 2024
Abstract
[125I] 2-(2,3-diiodo-4-hydroxyphenyl)-1,3,4-oxadiazole was synthesized (48% yield) and acid-hydrolyzed in situ with direct derivatization with p-nitro benzaldehyde to obtain the required 125I hydrazone (89% yield). A blood clearance kinetic study was performed on the 125I oxadiazole in a Sprague-Dawley rat and a biphasic behaviour was obtained. This study shows that 125I oxadiazole has potential to be metabolically stable and enough to allow imaging and tracking for a minimum of 2 h, making it a viable option for in situ indirect labeling of carbonyl containing macromolecules and keto steroids.
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- N. Klemm, S.-N. Su, B. Harnacker and I. Jeng, J. Labelled Comp. Radiopharm., 19, 937 (1982); https://doi.org/10.1002/jlcr.2580190806
- U. Braun, A.T. Shulgin, G. Braun and T. Sargent III, J. Med. Chem., 20, 1543 (1977); https://doi.org/10.1021/jm00222a001
- J. Boström, A. Hogner, A. Llinàs, E. Wellner and A.T. Plowright, J. Med. Chem., 55, 1817 (2012); https://doi.org/10.1021/jm2013248
- U.A. Atmaram and S.M. Roopan, Appl. Microbiol. Biotechnol., 106, 3489 (2022); https://doi.org/10.1007/s00253-022-11969-0
- P. Pitasse-Santos, V. Sueth-Santiago and M.E.F. Lima, J. Braz. Chem. Soc., 29, 435 (2018); https://doi.org/10.21577/0103-5053.20170208
- S.S. De, M.P. Khambete and M.S. Degani, Bioorg. Med. Chem. Lett., 29, 1999 (2019); https://doi.org/10.1016/j.bmcl.2019.06.054
- A.S. Peter Smith Derivatives of Hydrazine and other Hydronitrogens having N-N Bonds, Benjamin/Cummings Publishing Company, New York, p. 102 (1983).
- R.E. Counsell and R.D. Ice, in eds.: E.J. Ariens, The Design of Organ-Imaging Radiopharmaceuticals, In: Drug Design, Academic Press, NY, pp. 172-259 (1975).
- R.E. Counsell, B.H. Hong, R.E. Willette and V.V. Ranade, Steroids, 11, 817 (1968); https://doi.org/10.1016/S0039-128X(68)80096-0
- A.R. Fritzberg, in eds.: A.R. Fritzberg, Advances in Renal Radiopharma-ceuticals: In Radiopharmaceuticals: Progress and Clinical Perspectives, CRC Press, Boca Raton, FL, vol. I, p. 72 (1986).
References
N. Klemm, S.-N. Su, B. Harnacker and I. Jeng, J. Labelled Comp. Radiopharm., 19, 937 (1982); https://doi.org/10.1002/jlcr.2580190806
U. Braun, A.T. Shulgin, G. Braun and T. Sargent III, J. Med. Chem., 20, 1543 (1977); https://doi.org/10.1021/jm00222a001
J. Boström, A. Hogner, A. Llinàs, E. Wellner and A.T. Plowright, J. Med. Chem., 55, 1817 (2012); https://doi.org/10.1021/jm2013248
U.A. Atmaram and S.M. Roopan, Appl. Microbiol. Biotechnol., 106, 3489 (2022); https://doi.org/10.1007/s00253-022-11969-0
P. Pitasse-Santos, V. Sueth-Santiago and M.E.F. Lima, J. Braz. Chem. Soc., 29, 435 (2018); https://doi.org/10.21577/0103-5053.20170208
S.S. De, M.P. Khambete and M.S. Degani, Bioorg. Med. Chem. Lett., 29, 1999 (2019); https://doi.org/10.1016/j.bmcl.2019.06.054
A.S. Peter Smith Derivatives of Hydrazine and other Hydronitrogens having N-N Bonds, Benjamin/Cummings Publishing Company, New York, p. 102 (1983).
R.E. Counsell and R.D. Ice, in eds.: E.J. Ariens, The Design of Organ-Imaging Radiopharmaceuticals, In: Drug Design, Academic Press, NY, pp. 172-259 (1975).
R.E. Counsell, B.H. Hong, R.E. Willette and V.V. Ranade, Steroids, 11, 817 (1968); https://doi.org/10.1016/S0039-128X(68)80096-0
A.R. Fritzberg, in eds.: A.R. Fritzberg, Advances in Renal Radiopharma-ceuticals: In Radiopharmaceuticals: Progress and Clinical Perspectives, CRC Press, Boca Raton, FL, vol. I, p. 72 (1986).