Synthesis of 2-[ 123I and 124I]-iodoisonicotinic acid hydrazide—potential radiotracers for tuberculosis
The radiochemical syntheses of methyl 2-[ 123I]-iodoisonicotinate, 2-[ 123I]-iodoisonicotinic acid hydrazide and 2-[ 124I]-iodoisonicotinic acid hydrazide was accomplished. Iodine-123 was incorporated in the methyl ester molecule by an exchange reaction in glacial acetic acid. The average efficiency...
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| Published in | International journal of radiation applications and instrumentation. Part A, Applied radiation and isotopes Vol. 42; no. 3; pp. 215 - 220 |
|---|---|
| Main Authors | , , , |
| Format | Journal Article |
| Language | English |
| Published |
Oxford
Elsevier B.V
1991
Pergamon |
| Subjects | |
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| Abstract | The radiochemical syntheses of methyl 2-[
123I]-iodoisonicotinate, 2-[
123I]-iodoisonicotinic acid hydrazide and 2-[
124I]-iodoisonicotinic acid hydrazide was accomplished. Iodine-123 was incorporated in the methyl ester molecule by an exchange reaction in glacial acetic acid. The average efficiency of iodine exchange reaction was (92.6 ± 4.5)%. This radiotracer was extracted with ether and the solvent was evaporated. The residue was re-dissolved in anhydrous ethanol and treated with hydrazine under anhydrous conditions to obtain 2-[
123I]-iodoisonicotinic acid hydrazide. The overall radiochemical yield was 69%. Biodistribution data of both radio-tracers in male Sprague-Dawley rats were collected. This is the first report of SPECT radiopharmaceuticals which may be useful for differential diagnosis of intracranial masses (tuberculoma vs glioma), and CNS tuberculosis in immunosuppressed subjects. |
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| AbstractList | The radiochemical syntheses of methyl 2-[123I]-iodoisonicotinate, 2-[123I]-iodoisonicotinic acid hydrazide and 2-[124I]-iodoisonicotinic acid hydrazide was accomplished. Iodine-123 was incorporated in the methyl ester molecule by an exchange reaction in glacial acetic acid. The average efficiency of iodine exchange reaction was (92.6 +/- 4.5)%. This radiotracer was extracted with ether and the solvent was evaporated. The residue was re-dissolved in anhydrous ethanol and treated with hydrazine under anhydrous conditions to obtain 2-[123I]-iodoisonicotinic acid hydrazide. The overall radiochemical yield was 69%. Biodistribution data of both radio-tracers in male Sprague-Dawley rats were collected. This is the first report of SPECT radiopharmaceuticals which may be useful for differential diagnosis of intracranial masses (tuberculoma vs glioma), and CNS tuberculosis in immunosuppressed subjects. The radiochemical syntheses of methyl 2-[ 123I]-iodoisonicotinate, 2-[ 123I]-iodoisonicotinic acid hydrazide and 2-[ 124I]-iodoisonicotinic acid hydrazide was accomplished. Iodine-123 was incorporated in the methyl ester molecule by an exchange reaction in glacial acetic acid. The average efficiency of iodine exchange reaction was (92.6 ± 4.5)%. This radiotracer was extracted with ether and the solvent was evaporated. The residue was re-dissolved in anhydrous ethanol and treated with hydrazine under anhydrous conditions to obtain 2-[ 123I]-iodoisonicotinic acid hydrazide. The overall radiochemical yield was 69%. Biodistribution data of both radio-tracers in male Sprague-Dawley rats were collected. This is the first report of SPECT radiopharmaceuticals which may be useful for differential diagnosis of intracranial masses (tuberculoma vs glioma), and CNS tuberculosis in immunosuppressed subjects. |
| Author | Lambrecht, R.M. Sajjad, M. Somawardhana, C.W. Amartey, J.K. |
| Author_xml | – sequence: 1 givenname: C.W. surname: Somawardhana fullname: Somawardhana, C.W. organization: Radionuclide and Cyclotron Operations Department, King Faisal Specialist Hospital and Research Centre, P.O. Box 3354, Riyadh 11211, Kingdom Saudi Arabia – sequence: 2 givenname: M. surname: Sajjad fullname: Sajjad, M. – sequence: 3 givenname: J.K. surname: Amartey fullname: Amartey, J.K. – sequence: 4 givenname: R.M. surname: Lambrecht fullname: Lambrecht, R.M. |
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| Cites_doi | 10.1002/cber.19620950526 10.3171/jns.1968.29.2.0149 10.1146/annurev.pa.26.040186.001151 10.2105/AJPH.70.9.987 10.1524/ract.1990.50.12.123 10.1021/je60059a039 10.3171/jns.1970.33.2.0203 10.1248/yakushi1947.81.4_574 10.1021/jm00226a007 10.1021/ja01104a046 10.3171/jns.1961.18.1.0001 10.1016/0883-2889(89)90211-6 10.1001/jama.1985.03350270091029 10.1007/BF01742762 10.1093/brain/88.2.375 10.1016/0883-2889(91)90162-T 10.1016/0168-9002(89)90156-3 10.2214/ajr.130.4.769 10.7326/0003-4819-105-2-210 |
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| Keywords | Organic hydrazide Iodine Isotopes Nitrogen heterocycle Labelled compound Halogen Organic compounds |
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| Snippet | The radiochemical syntheses of methyl 2-[
123I]-iodoisonicotinate, 2-[
123I]-iodoisonicotinic acid hydrazide and 2-[
124I]-iodoisonicotinic acid hydrazide was... The radiochemical syntheses of methyl 2-[123I]-iodoisonicotinate, 2-[123I]-iodoisonicotinic acid hydrazide and 2-[124I]-iodoisonicotinic acid hydrazide was... |
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| SubjectTerms | Animals Biological Availability Brain Diseases - diagnostic imaging Chemistry Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with only one n hetero atom and condensed derivatives Iodine Radioisotopes Isoniazid - analogs & derivatives Isoniazid - chemical synthesis Isoniazid - pharmacokinetics Isonicotinic Acids - chemical synthesis Isonicotinic Acids - pharmacokinetics Isotope Labeling - methods Male Organic chemistry Preparations and properties Radiochemistry Radionuclide Imaging Rats Rats, Inbred Strains Tuberculoma - diagnostic imaging |
| Title | Synthesis of 2-[ 123I and 124I]-iodoisonicotinic acid hydrazide—potential radiotracers for tuberculosis |
| URI | https://dx.doi.org/10.1016/0883-2889(91)90079-G https://www.ncbi.nlm.nih.gov/pubmed/1647381 |
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