Development of novel derivatives of imino sugar and thio sugar for drug discovery
| Project/Area Number |
18K06553
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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| Research Institution | Tohoku Medical and Pharmaceutical University |
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Principal Investigator |
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| Project Period (FY) |
2018-04-01 – 2022-03-31
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| Project Status |
Completed (Fiscal Year 2021)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2021: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2020: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2019: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2018: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
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| Keywords | イミノ糖 / チオ糖 / 酵素阻害活性 / 構造活性相関 / 不斉合成 / 複素環化合物 / ピペリジン環 / ピロリジン環 / α-グルコシダーゼ阻害活性 / 超原子価ヨウ素 / 生理活性物質 / 創薬化学 |
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| Outline of Final Research Achievements |
In this study, the syntheses of new iminosugars and thiosugars were investigated. Synthesis of new iminosugar derivatives was investigated by several methods, including cyclization using diphenyl diselenide, multiple metal catalysts, and chiral pooling method. In the study of thiosugar, the synthesis of thiofuranose derivatives from thioepoxide by cyclization via episulfonium ions was also investigated.
Furthermore, the obtained compounds were evaluated for biological activity and the results were published in several papers.
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| Academic Significance and Societal Importance of the Research Achievements |
学術的意義；これまでに開発されていないイミノ糖・チオ糖の新しい合成法を生み出すことが可能となる。さらにそれらの酵素への影響を解明できる。
社会的意義；糖は、エネルギー源となるだけでなく、核酸の構成成分、タンパク質や脂質に含まれる糖鎖として幅広く活用されている。そのため糖の代謝、糖鎖の形成に関与する酵素をコントロールできるイミノ糖・チオ糖を創出することで、これまでに治療薬がない病気の医薬品開発に貢献できる。
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Report
(5 results)
Research Products
(18 results)
