
Journal of Medicinal Chemistry p. 8866 - 8872 (2019)
Update date:2022-08-11
Topics:
Chen, Zhen
Mori, Wakana
Fu, Hualong
Schafroth, Michael A.
Hatori, Akiko
Shao, Tuo
Zhang, Genwei
Van, Richard S.
Zhang, Yiding
Hu, Kuan
Fujinaga, Masayuki
Wang, Lu
Belov, Vasily
Ogasawara, Daisuke
Giffenig, Pilar
Deng, Xiaoyun
Rong, Jian
Yu, Qingzhen
Zhang, Xiaofei
Papisov, Mikhail I.
Shao, Yihan
Collier, Thomas L.
Ma, Jun-An
Cravatt, Benjamin F.
Josephson, Lee
Zhang, Ming-Rong
Liang, Steven H.
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.
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Doi:10.1016/j.jinorgbio.2016.04.002
(2016)Doi:10.1515/mgmc-2012-0010
(2012)Doi:10.1039/c5ta10713j
(2016)Doi:10.1007/s00726-020-02846-z
(2020)Doi:10.1016/j.tetlet.2017.06.055
(2017)Doi:10.1016/0223-5234(91)90153-E
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