| Project/Area Number |
23590137
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Multi-year Fund |
|---|
| Section | 一般 |
|---|
| Research Field |
Drug development chemistry
|
|---|
| Research Institution | Kobe Pharmaceutical University (2014)
Kobe Gakuin University (2011-2013) |
|---|
Principal Investigator |
HAMADA Yoshio 神戸薬科大学, 薬学部, 研究員 (70424968)
|
|---|
| Project Period (FY) |
2011-04-28 – 2015-03-31
|
| Project Status |
Completed (Fiscal Year 2014)
|
| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2013: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2012: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2011: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
|
|---|
| Keywords | アルツハイマー病 / BACE1 / β-セクレターゼ / 酵素阻害剤 / ペプチド / アミロイドβ / 凝集阻害剤 / アミロイドβペプチド / 阻害剤 米国 |
|---|
| Outline of Final Research Achievements |
The increase of dementia patients is a big issue for Japan as it faces a rapidly aging society. To conquer Alzheimer’s disease, this research project aimed the development of BACE1 and Aβ aggregation inhibitors. Novel BACE1 inhibitors, YHI-309 and YHI-764 (IC50 = 13 nM and 26 nM, respectively), with a nitro or thiadiazole group were designed and synthesized. These compounds appear to have promise as drug candidates because of their increased membrane permeability.
Aβ aggregation inhibitors, YHI-008 and YHI-009, also designed and synthesized. These compounds exhibited potent inhibitory activity against the Aβ aggregation, and could recognize a specific Aβ conformer. These compounds are expected to use a research tool for pathogenic mechanism analysis.
|
