| アイテムタイプ |
学術雑誌論文 / Journal Article(1) |
| 公開日 |
2024-09-02 |
| タイトル |
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タイトル |
Synthesis and structure?activity relationship (SAR) studies of 1,2,3-triazole, amide, and ester-based benzothiazole derivatives as potential molecular probes for tau protein |
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言語 |
en |
| 言語 |
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言語 |
eng |
| 資源タイプ |
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資源タイプ識別子 |
http://purl.org/coar/resource_type/c_6501 |
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資源タイプ |
journal article |
| 著者 |
Hendris Wongso
Ono Maiko
Yamasaki Tomoteru
Kumata Katsushi
Higuchi Makoto
Zhang Ming-Rong
Michael J. Fulham
Andrew Katsifis
Paul A. Keller
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| 抄録 |
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内容記述タイプ |
Abstract |
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内容記述 |
The pyridinyl-butadienyl-benzothiazole (PBB3 15) scaffold was used to develop tau ligands with improved in vitro and in vivo properties for imaging applications to provide insights into the etiology and characteristics of Alzheimer's disease. The photoisomerisable trans-butadiene bridge of PBB3 was replaced with 1,2,3-triazole, amide, and ester moieties and in vitro fluorescence staining studies revealed that triazole derivatives showed good visualisation of Aβ plaques, but failed to detect the neurofibrillary tangles (NFTs) in human brain sections. However, NFTs could be observed using the amide 110 and ester 129. Furthermore, the ligands showed low to high affinities (Ki = >1.5 mM?0.46 nM) at the shared binding site(s) with PBB3. |
| 書誌情報 |
RSC Medicinal Chemistry
巻 14,
号 5,
p. 858-868,
発行日 2023-01
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| 出版者 |
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出版者 |
Royal Society of Chemistry |
| ISSN |
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収録物識別子タイプ |
ISSN |
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収録物識別子 |
2040-2503 |
| DOI |
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識別子タイプ |
DOI |
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関連識別子 |
10.1039/D2MD00358A |
