Design, Synthesis, and Evaluation of 18F‑Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes
收藏Figshare2019-09-13 更新2026-04-29 收录
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https://figshare.com/articles/dataset/Design_Synthesis_and_Evaluation_of_sup_18_sup_F_Labeled_Monoacylglycerol_Lipase_Inhibitors_as_Novel_Positron_Emission_Tomography_Probes/9911378
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Dysfunction of monoacylglycerol lipase (MAGL) is associated with several psychopathological disorders, including drug addiction and neurodegenerative diseases. Herein we design, synthesize, and evaluate several irreversible fluorine-containing MAGL inhibitors for positron emission tomography (PET) ligand development. Compound 6 (identified from a therapeutic agent) was advanced for 18F-labeling via a novel spirocyclic iodonium ylide (SCIDY) strategy, which demonstrated high brain permeability and excellent specific binding. This work supports further development of novel 18F-labeled MAGL PET probes.
创建时间:
2019-09-13



