Asymmetric syntheses of various iminofuranoses having a side chain at C1 position and their biological evaluation as enzyme inhibitors
| Project/Area Number |
25860088
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Drug development chemistry
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| Research Institution | Tohoku Pharmaceutical University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
TAKAHATA Hiroki 東北薬科大学, 薬学部, 教授 (00109109)
YOSHIMURA Yuichi 東北薬科大学, 薬学部, 教授 (00230813)
KATO Atsushi 富山大学, 付属病院薬剤部, 准教授 (60303236)
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| Project Period (FY) |
2013-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Keywords | 医薬品化学 / イミノ糖 / 医薬分子設計 / 酵素阻害活性物質 / α-グルコシダーゼ阻害薬 / ゴーシェ病治療薬 / ケミカルシャペロン療法 / イミノ糖誘導体 / ライソゾーム病 / 化学シャペロン療法 / 構造活性相関研究 |
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| Outline of Final Research Achievements |
This research program aimed at developing new potent and selective glucosidase inhibitors. I have focused on the α-1-C-substituted L- and D- iminofuranose derivatives.The asymmetric syntheses of α-1-C-alkyl D- and L-iminofuranose derivatives were achieved. Their inhibitory activities were measured.
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Report
(4 results)
Research Products
(15 results)
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[Journal Article] Docking study and biological evaluation of pyrrolidine-based iminosugars as pharmacological chaperones for Gaucher disease2016
Author(s)
Atsushi Kato, Izumi Nakagome, Kasumi Sato, Arisa Yamamoto, Isao Adachi, Robert J. Nash, George W. J. Fleet, Yoshihiro Natori, Yasuka Wasuka, Tatsushi Imahori, Yuichi Yoshimura, Hiroki Takahata and Shuichi Hirono
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Journal Title
Org. Bio. Chem.
Volume: 14
Issue: 3
Pages: 1039-1048
DOI
Related Report
Peer Reviewed / Open Access / Int'l Joint Research
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