A new 18F-labelled derivative of the MMP inhibitor CGS 27023A for PET: Radiosynthesis and initial small-animal PET studies |
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| Affiliation: | 2. Department of Diagnostic and Therapeutic Neuroradiology, Hôpital Foch Suresnes FR, University of Versailles Saint Quentin-en-Yvelines, France;3. Department of Neuroradiology, S. Anna Hospital, Ferrara, Italy;4. Department of Interventional Neuroradiology, Rothschild Foundation hospital, Paris, France;5. Department of Neurology, Hôpital Foch Suresnes FR, University of Versailles Saint Quentin-en-Yvelines, France;1. Eskisehir Osmangazi University, Medical Faculty, Department of Neurology, Neurocritical Care, Cerebrovascular Disease, Interventional Neurology, Eskisehir, Turkey;2. Gaziantep University, Medical Faculty, Department of Neurology, Interventional Neurology, Turkey;3. Eskisehir Osmangazi University, Medical Faculty, Department of Neurology, Neurocritical Care, Cerebrovascular Disease, Interventional Neurology 26040 Eskisehir, Turkey;4. Gaziantep University, Medical Faculty, Department of Neurology, Turkey;5. Baskent University, Medical Faculty, Department of Neurology, Ankara, Turkey;6. Harran University, Medical Faculty, Department of Neurology, Turkey |
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| Abstract: | The CGS 27023A derivative (R)-2-(N-((6-fluoropyridin-3-yl)methyl)-4-methoxyphenyl-sulphonamido)-N-hydroxy-3-methylbutanamide 1a was identified as a very potent matrix metalloproteinase inhibitor. Here, we describe a one-step radiosynthesis of the target compound [18F]1a. The syntheses of [18F]1a resulted in a radiochemical yield of 12.1±5.9% (decay-corrected), a radiochemical purity of 98.8±0.6%, and a specific activity of 39±27 GBq/μmol at the end of synthesis within 160±18 min from the end of radionuclide production (n=5). Initial small-animal PET studies in wild-type mice (C57/BL6) showed no unfavourable tissue accumulation of [18F]1a. |
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