- Synthesis of an iodine-123-labeled celecoxib analogue: A potential spect agent
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Celecoxib (4[5-(4-methylphenyl)-3-(trifluoromethy)-1H-pyrazol-1yl]- benzenesulfonamide) is an effective inhibitor of the cyclooxygenase-2 (COX-2). The synthesis of a no-carrier-added iodine-123-labeled analogue of celecoxib was accomplished in four steps for potential use in single photon tomography. Copyright
- Kabalka, George W.,Mereddy, Arjun R.,Schuller, Hildegard M.
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- Isotope labelling by reduction of nitriles: Application to the synthesis of isotopologues of tolmetin and celecoxib
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The aryl methyl group is found in many drug-like compounds, but there are limited ways of preparing compounds with an isotope label in this methyl position. The process of cyanation of an aryl halide followed by complete reduction of the nitrile to a methyl group was investigated as a route for preparing stable and radiolabelled isotopologues of drug-like compounds. Using this methodology, carbon-13, deuterium, carbon-14, and tritium labelled isotopologues of the nonsteroidal anti-inflammatory drug tolmetin were produced, as well as carbon-13, deuterium, and carbon-14 labelled isotopologues of another nonsteroidal anti-inflammatory drug, celecoxib. The radiolabelled compounds were produced at high specific activity and the stable isotope labelled compounds with high incorporation making them suitable for use as internal standards in mass spectrometry assays. This approach provides a common synthetic route to multiple isotopologues of compounds using inexpensive and readily available labelled starting materials.
- Ellis-Sawyer, Kate,Bragg, Ryan A.,Bushby, Nick,Elmore, Charles S.,Hickey, Michael J.
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p. 213 - 220
(2017/04/10)
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- HETEROCYCLES USEFUL AS INHIBITORS OF CARBONIC ANHYDRASE
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Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.
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(2008/06/13)
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- Diagnosis of diseases associated with COX-2 expression
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Derivatives of cyclooxygenase-2 inhibitor compounds are made incorporating a label that can be identified upon administration into the body of a mammal and subsequent binding of the compounds with cyclooxygenase-2 that is overexpressed due to a disease co
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Page/Page column 4
(2008/06/13)
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