Dataset Information

Design, Synthesis, and Evaluation of ¹⁸F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.

ABSTRACT: 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.

SUBMITTER: Chen Z

PROVIDER: S-EPMC7875603 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Evaluation of 18F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.

Chen Zhen Z Mori Wakana W Fu Hualong H Schafroth Michael A MA Hatori Akiko A Shao Tuo T Zhang Genwei G Van Richard S RS Zhang Yiding Y Hu Kuan K Fujinaga Masayuki M Wang Lu L Belov Vasily V Ogasawara Daisuke D Giffenig Pilar P Deng Xiaoyun X Rong Jian J Yu Qingzhen Q Zhang Xiaofei X Papisov Mikhail I MI Shao Yihan Y Collier Thomas L TL Ma Jun-An JA Cravatt Benjamin F BF Josephson Lee L Zhang Ming-Rong MR Liang Steven H SH

Journal of medicinal chemistry 20190926 19

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 bra ...[more]

PMID: 31518130

Dataset Information

Design, Synthesis, and Evaluation of ¹⁸F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.

Publications

Design, Synthesis, and Evaluation of <sup>18</sup>F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.

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