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Synthesis, radioiodination and in vivo evaluation of ethyl 1,4-dihydro-7-iodo-4-oxoquinoline-3-carboxylate as a potential pulmonary perfusion scintigraphic radiopharmaceutical

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Abstract

The goal of this study was to biologically evaluate a newly synthesized radioiodinated ethyl 1,4-dihydro-7-iodo-4-oxoquinoline-3-carboxylate (EIOQC) as a potential lung scintigraphic agent. EIOQC was synthesized, characterized then radioiodinated via direct electrophilic substitution reaction. Factors affecting the radiochemical purity were studied in details and the biological distribution of the radioiodinated compound was evaluated in normal male Albino mice. EIOQC was successfully synthesized and radioiodinated with high radiochemical purity (96 ± 1.21 %) and in vitro stability up to 48 h. The biological evaluation of radioiodinated EIOQC showed high lung affinity of 21.36 ± 1.73 % injected dose/g organ (% ID/g) at 15 min. This study introduces radioiodinated EIOQC as a novel potential radiopharmaceutical for lung perfusion scintigraphy.

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Acknowledgments

The authors are grateful to Prof. Dr. Detlef Geffken for his help in the organic synthesis of EIOQC.

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Authors and Affiliations

  1. Radioactive Isotopes and Generator Department, Hot Labs Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    T. M. Sakr

  2. Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt

    M. A. Motaleb

  3. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Helwan University, Cairo, Egypt

    W. A. Zaghary

Authors
  1. T. M. Sakr
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  2. M. A. Motaleb
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  3. W. A. Zaghary
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Correspondence to T. M. Sakr.

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Sakr, T.M., Motaleb, M.A. & Zaghary, W.A. Synthesis, radioiodination and in vivo evaluation of ethyl 1,4-dihydro-7-iodo-4-oxoquinoline-3-carboxylate as a potential pulmonary perfusion scintigraphic radiopharmaceutical. J Radioanal Nucl Chem 303, 399–406 (2015). https://doi.org/10.1007/s10967-014-3299-3

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  • DOI: https://doi.org/10.1007/s10967-014-3299-3

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