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Structural design of glutamate transporter 18F-PET agent and synthesis using a Click-Reaction
https://repo.qst.go.jp/records/84496
https://repo.qst.go.jp/records/844969d5ff608-444e-4094-8962-1893584f12fa
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2022-01-05 | |||||
| タイトル | ||||||
| タイトル | Structural design of glutamate transporter 18F-PET agent and synthesis using a Click-Reaction | |||||
| 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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 |
Hiroshi, Yamaguchi
× Hiroshi, Yamaguchi× Yamashiro, Keiichi× Maki, Okada× Karuo, Yukiko× Omote, Masaaki× Kato, Katsuhiko× Hiroshi, Yamaguchi× Maki, Okada |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Background and purpose We excelled off-target binding using computer chemistry techniques and worked on the development of PET imaging agents that bind to glutamate transporter (GLT). Although a plurality of asymmetric carbons generated within the compound skeleton could be excluded by structure optimization, there was a problem with deprotection of the aspartic acid skeleton in the skeleton. This study aims at establishing synthesis reactions that do not require protection / deprotection reaction by Click-Reaction, recalculation of In Silico binding assay, and synthesis of obtained structural compounds. Method In silico binding assay we derive the predominant and ERα non-binding structure in GLT binding and have studied labeling by [18F] on synthesis and synthesizer. In the structure reported earlier, there was a problem in deprotection of the aspartic acid skeleton in the skeleton. We examined the establishment of synthetic reactions that do not require protection / deprotection reaction by Click-Reaction. Results and discussion We have established a design and synthesis route for compounds excluding asymmetric positions. However, as the yield in the deprotection reaction was low, a synthesis reaction that did not require protection / deprotection reaction by Click-Reaction was established. At present, the labeling reaction is preparing for sequencing at the time of synthesis, label synthesis, and animal experiments. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | The 2021 International Chemical Congress of Pacific Basin Societies (Pacifichem 2021) | |||||
| 発表年月日 | ||||||
| 日付 | 2021-12-19 | |||||
| 日付タイプ | Issued | |||||
