Abstract
Fluoroalkyl and fluoroaryl analogues of valdecoxib were found to possess potent inhibitory activities against cyclooxygenase-2 comparable to that of the parent valdecoxib. Among them, the fluoromethyl analogue was chosen for 18F-labeling. Thus, 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide (approximately 2000 Ci/mmol at end of synthesis) was synthesized by [18F]fluoride-ion displacement of the corresponding tosylate in approximately 40% decay-corrected radiochemical yield within approximately 120 min from end of bombardment.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Cyclooxygenase Inhibitors* / chemical synthesis
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Cyclooxygenase Inhibitors* / pharmacokinetics
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Fluorine Radioisotopes / pharmacokinetics
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Humans
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Inhibitory Concentration 50
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Isoxazoles / chemical synthesis*
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Macrophages / enzymology
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Mice
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Positron-Emission Tomography / methods*
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / pharmacokinetics
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Tissue Distribution
Substances
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4-(5-(18F)fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide
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Cyclooxygenase Inhibitors
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Fluorine Radioisotopes
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Isoxazoles
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Radiopharmaceuticals
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Sulfonamides
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valdecoxib