当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Design, Synthesis, and Evaluation of 18F-Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes.

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Chen Z,Mori W,Fu H,Schafroth MA,Hatori A,Shao T,Zhang G,Van RS,Zhang Y,Hu K,Fujinaga M,Wang L,Belov V,Ogasawara D,Giffenig P,Deng X,Rong J,Yu Q,Zhang X,Papisov MI,Shao Y,Collier TL,Ma JA,Cravatt BF,Josephs

doi

10.1021/acs.jmedchem.9b00936

subject

Has Abstract

pub_date

2019-10-10 00:00:00

pages

8866-8872

issue

19

eissn

0022-2623

issn

1520-4804

journal_volume

62

pub_type

杂志文章

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