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Design, Synthesis, and Evaluation of 18F‑Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes
https://repo.qst.go.jp/records/77720
https://repo.qst.go.jp/records/77720384b6eb6-419e-42a8-b2b0-bedd6584a486
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2019-11-28 | |||||
| タイトル | ||||||
| タイトル | Design, Synthesis, and Evaluation of 18F‑Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Chen, Zhen
× Chen, Zhen× Mori, Wakana× Fu, Hualong× A. Schafroth, Michael× Hatori, Akiko× Shao, Tuo× Zhang, Genwei× S. Van, Richard× Zhang, Yiding× Hu, Kuan× Fujinaga, Masayuki× Ming-Rong, Zhang× Wakana, Mori× Akiko, Hatori× Zhang, Yiding× Kuan, Hu× Masayuki, Fujinaga× Zhang, Ming-Rong |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 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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| 書誌情報 |
Journal of Medicinal Chemistry 巻 62, 号 19, p. 8866-8872, 発行日 2019-09 |
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| 出版者 | ||||||
| 出版者 | ACS | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/acs.jmedchem.9b00936 | |||||
| 関連サイト | ||||||
| 識別子タイプ | URI | |||||
| 関連識別子 | https://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.9b00936 | |||||
