| Project/Area Number |
25860093
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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 | Kyoto Pharmaceutical University |
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Principal Investigator |
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| Co-Investigator(Renkei-kenkyūsha) |
AKAJI Kenichi 京都薬科大学, 薬学部, 教授 (60142296)
HATTORI Yasunao 京都薬科大学, 薬学部, 助教 (20567028)
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| Research Collaborator |
DEGUCHI Ayaka 京都薬科大学, 薬学部
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| Project Period (FY) |
2013-04-01 – 2015-03-31
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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2014: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2013: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
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| Keywords | アルツハイマー病 / BACE1 / ヒドロキシエチルアミン / 遷移状態アナログ / 閉環メタセシス |
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| Outline of Final Research Achievements |
I have investigated to develop novel β-secretase (BACE1) inhibitors for treatment of Alzheimer’s disease. Our structure-activity relationship study for P1’ site of hydroxyethylamine (HEA)-type BACE1 inhibitors, which were designed based on the substrate sequence, identified an optimum structure of HEA unit. Furthermore, in our study for improvement of their activity and bioavailability using bridged structure, a bridged BACE1 inhibitor was identified by MS spectrometer.
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