1. Green synthesis, radioiodination and in vivo biodistribution of 5-(2-hydroxyphenyl)-2,4-dihydro-3H-pyrazol-3-one derivatives as potential candidates for lung imaging.
- Author
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Abdou, Moaz M., Gizawy, Mohamed A., and Shamsel-Din, Hesham A.
- Subjects
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RADIOIODINATION , *COUMARINS , *LUNGS , *RADIOCHEMICAL purification , *MALTOSE , *CHEMICAL yield , *PYRAZOLE derivatives , *HYDRAZINE - Abstract
Lung targeting was developed by synthesising pyrazolone derivatives 6a-f under solvent-free and thermal conditions by reacting azo coumarins 4a-c with hydrazines 5a and b using maltose as a biodegradable catalyst. Different spectral data characterized the synthesized agents as proton-NMR, FT-IR, and mass spectra. Direct radioiodination with iodine-131 was performed and optimized to reach the highest radiochemical purities (92 ± 0.47 to 98 ± 0.21%) using chloramine-T, a moderate oxidizing agent. The 131I-pyrazolone derivatives were confirmed based on HRMS. Furthermore, radioiodinated nitro-derivatives accumulated well in the lung of normal mice during in vivo evaluation, and the better uptake was for nitrophenyl-derivative 7f, about 30.06 ± 0.04% at 30 min after injection. Consequently, synthesized radioiodinated derivatives may be employed as prospective tracers for lung perfusion scans. • Synthesis and radiolabeling of a new pyrazole derivatives were done. • The effect of various reaction conditions on the percent radiochemical yield of radiolabeled derivative was studied. • The in vivo bioevaluation in normal mice showed good accumulation of radioiodinated pyrazole derivative in lung. • The synthetized pyrazole could be used as a potential lung imaging agents. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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