2014 Fiscal Year Final Research Report
Development of amyloid beta aggregation inhibitor for therapeutics of Alzheimer disease
| Project/Area Number |
24590147
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Teikyo Heisei University (2014)
Toho University (2012-2013) |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
ISHIGAMI Akihito 地方独立行政法人東京都健康長寿医療センター(東京都健康長寿医療センター研究所), 東京都健康長寿医療センター研究所, 研究副部長 (50270658)
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| Project Period (FY) |
2012-04-01 – 2015-03-31
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| Keywords | アルツハイマー / アミロイドベータ / 凝集阻害剤 / 繊維化阻害剤 / ベンゾフラン / グルコサミン酸 / 多価フェノール / 有機合成 |
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| Outline of Final Research Achievements |
We thought aggregation inhibitor of amyloid beta would be a prophylactic agent for Alzheimer diseases, furthermore disrupting compound for the aggregation, it would be a therapeutic medication. To inhibit Amyloid-β (Aβ) aggregation/fibril formation, we have found a concept that an Aβ-recognition compound attached to the hydrophilic moiety act as a strong Aβ-aggregation inhibitor. Many phenolic derivatives of 2, 5-diarylbenzofuran are synthesized according to our concept. Some poly-hydric phenol derivatives showed strong activities for Aβ aggregation and fibril formation inhibitory activity and dissociation activity for Aβ fibrils and aggregates. These activities are obviously related to the number of hydroxyl groups in the structures. Viewing from the Log P values of structures, the compounds having around Log P=4 values are showed the most strong activities. From the molecular weight and Log P values, these strong inhibitors would be expected to cross the BBB.
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| Free Research Field |
医薬品化学
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