2016 Fiscal Year Final Research Report
Development of novel BACE1 inhibitors based on the N-amidino nitrogen-containing ring structure
| Project/Area Number |
15K18902
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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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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Keywords | アルツハイマー病 / BACE1 / 低分子阻害剤 / アミジノ基 / ピロリジン / ピペリジン |
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| Outline of Final Research Achievements |
I have investigated to develop novel small molecule β-secretase (BACE1) inhibitors based on an N-amidino nitrogen-containing ring structure. Focusing on amidino-pyrrolidine and amidino-piperidine as the structure, I synthesized several derivatives, and evaluated their BACE1 inhibitory activity. The structure-activity relationship study suggested that two balky substituents located on a five- or six-ring structure with trans-configuration contributed to the bioactivity.
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| Free Research Field |
創薬科学
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