2014 Fiscal Year Final Research Report
Development of novel BACE1 inhibitors: Structure activity relationship study based on the substrate sequence
| 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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| 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 |
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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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| Free Research Field |
メディシナルケミストリー
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