Development of Novel Tau Protein-Binding Compounds Based on the Alkene-to-Chloroalkene Isosteric Switch Strategy
| Project/Area Number |
16K15142
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Shizuoka University |
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Principal Investigator |
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| Project Period (FY) |
2016-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | PET薬剤 / タウタンパク質 / 神経原繊維変化 / PBB3 / 薬学 |
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| Outline of Final Research Achievements |
As part of a program aimed at identifying the utility of haloalkene-containing molecules, synthetic and evaluation studies of chloroalkene-conjugated PBB3 derivative, ITY11-397, were performed for the development of novel tau-imaging PET tracers with improved operability. ITY11-397 was designed based on the alkene-to-chloroalkene isosteric switching strategy and can be prepared in 8 steps from 2-chloro-5-cyanopyridine. Evaluation study on the photostability revealed that the photostability of ITY11-397 is 6-fold higher than that of the corresponding unsubstituted compound. In addition, ITY11-397 showed higher binding selectivity to the 2N3R-type Tau protein. The main advantage of such chloroalkene-conjugated systems lies in their simple chemical modification, making possible the application of this strategy to various molecules with acyclic conjugated system(s), which should contribute to the development of photoresistant molecules with conjugated system(s).
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Report
(3 results)
Research Products
(17 results)
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[Journal Article] The Role of Chemisorption for Push-Pull Chromophores on SiO2 Surfaces in Non-Electrically Poling Host-Guest NLO Polymers2017
Author(s)
Atsushi Sugita, Kazuma Ito, Yasuaki Sato, Ryota Suzuki, Kohei Sato, Tetsuo Narumi, Nobuyuki Mase, Yasushi Takano, Tomonori Matsushita, Shigeru Tasaka, and Yoshimasa Kawata
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Journal Title
Journal of Photochemistry and Photobiology A: Chemistry
Volume: 340
Pages: 35-45
DOI
Related Report
Peer Reviewed / Acknowledgement Compliant
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[Journal Article] Synthesis of a self-assembling gold nanoparticle-supported organocatalyst for enamine-based asymmetric aldol reactions.2016
Author(s)
Soti, P.Z., Yamashita,H., Sato,K., Narumi, T., Toda, M., Watanabe, N., Marosi,G., Mase, N.
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Journal Title
Tetrahedron
Volume: 72
Issue: 16
Pages: 1984-1990
DOI
NAID
Related Report
Peer Reviewed / Open Access / Int'l Joint Research
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