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完整後設資料紀錄
DC 欄位 | 值 | 語言 |
---|---|---|
dc.contributor.advisor | 忻凌偉(Ling-Wei Hsin) | |
dc.contributor.author | Shu-Cheng Chou | en |
dc.contributor.author | 周書呈 | zh_TW |
dc.date.accessioned | 2021-06-08T01:45:04Z | - |
dc.date.copyright | 2016-08-26 | |
dc.date.issued | 2016 | |
dc.date.submitted | 2016-08-15 | |
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PYRROC: the first functionalized cycloalkyne that facilitates isomer-free generation of organic molecules by SPAAC. Organic & biomolecular chemistry 2015, 13 (13), 3866-3870. 40. Lee, J. C.; Francis, S.; Dutta, D.; Gupta, V.; Yang, Y.; Zhu, J.-Y.; Tash, J. S.; Schönbrunn, E.; Georg, G. I. Synthesis and Evaluation of Eight- and Four-Membered Iminosugar Analogues as Inhibitors of Testicular Ceramide-Specific Glucosyltransferase, Testicular β-Glucosidase 2, and Other Glycosidases. The Journal of Organic Chemistry 2012, 77 (7), 3082-3098. | |
dc.identifier.uri | http://tdr.lib.ntu.edu.tw/jspui/handle/123456789/19100 | - |
dc.description.abstract | Tau protein is a microtubule-related proteins which was found in the neurons of the central nervous system. Its role is to stabilize the structure of the microtubules of the neurons. Abnormal degeneration of the tau protein often leads to dysfunction and causes several neurodegenerative disorders, such as Alzheimer’s disease. 7-(6-Fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole ([18F]T807) is a potential tau protein molecular imaging probe for positron emission tomography (PET). In this study, the precursor 8 for radiosynthesis of [18F]T807 was synthesized using 3-bromopyridine as starting material. The overall chemical yield was increased from 8% to 17% through the optimization process. N-Alkylation of pyrido[4,3-b]indole 6 with appropriate alkyl halides yielded compounds 11a-c, 14 and 17. Treatment of 11a-c, 14 and 17 with boronic ether or acid under Suzuki reaction condition yielded nitro precursors 12a-c and the fluoro-substituted standards 13a-c and 15. In this series, the log D values of 13a-c and 15 were within the desired range for blood-brain barrier penetration (2.0 ≤ log D ≤ 3.5). All compounds possessed high blood brain barrier penetration potential (Pe ≥ 10 × 10-6 cm/s) in PAMPA assay. These compounds are now being investigated as novel Tau protein PET radiotracer in collaboration with Department of Nuclear medicine, National Taiwan University Hospital. | en |
dc.description.provenance | Made available in DSpace on 2021-06-08T01:45:04Z (GMT). No. of bitstreams: 1 ntu-105-R03423020-1.pdf: 7113488 bytes, checksum: 7dad58d672eb6c00e8f144edf0e84c32 (MD5) Previous issue date: 2016 | en |
dc.description.tableofcontents | 口試委員會審定書 I
誌謝 II 中文摘要 III Abstract IV 目錄 V 圖目錄 VII 表目錄 VIII 路徑目錄 IX 英文縮寫表 X Chapter 1 緒論 1 1.1 阿茲海默症(Alzheimer’s disease)的簡介 1 1.1.1 阿茲海默症的症狀 1 1.1.2 阿茲海默症的成因 2 1.2 正子造影和核種的使用 3 1.3 正子造影應用於阿茲海默症 5 Chapter 2 研究目的 8 Chapter 3 結果與討論 9 3.1 合成T807的前驅物和標準品 9 3.1.1 化合物2, 3, 4之合成 9 3.1.2 化合物5, 6之合成 10 3.1.3 化合物7, 8, 9, 10之合成 12 3.2 合成T807衍生物的前驅物和標準品 13 3.2.1 合成N-alkylation的衍生物 14 3.2.2 合成標定在N-alkylation的衍生物 15 3.2.3 化合物12b之放射性標定與正子造影 18 3.3 物化性質測定 24 Chapter 4 結論 31 實驗部分 32 1. 實驗藥品及溶劑來源 32 1.1 藥品及溶劑 32 1.2 自製無水溶劑 34 2. 實驗儀器裝置 34 3. 合成步驟與數據分析 36 參考文獻 61 附圖 67 | |
dc.language.iso | zh-TW | |
dc.title | 開發具診斷阿茲海默症潛力的新穎分子探針 | zh_TW |
dc.title | Discovery of Novel Molecular Probe for Diagnosis of
Alzheimer’s Disease | en |
dc.type | Thesis | |
dc.date.schoolyear | 104-2 | |
dc.description.degree | 碩士 | |
dc.contributor.oralexamcommittee | 王光昭(Guang-Zhao Wang),陳基旺(Ji-Wang Chern),梁碧惠(Pi-Hui Liang) | |
dc.subject.keyword | 阿茲海默症, | zh_TW |
dc.subject.keyword | NULL | en |
dc.relation.page | 110 | |
dc.identifier.doi | 10.6342/NTU201602334 | |
dc.rights.note | 未授權 | |
dc.date.accepted | 2016-08-15 | |
dc.contributor.author-college | 醫學院 | zh_TW |
dc.contributor.author-dept | 藥學研究所 | zh_TW |
顯示於系所單位: | 藥學系 |
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