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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| Project Status |
Completed (Fiscal Year 2014)
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| Budget Amount *help |
¥5,330,000 (Direct Cost: ¥4,100,000、Indirect Cost: ¥1,230,000)
Fiscal Year 2014: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2013: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2012: ¥2,860,000 (Direct Cost: ¥2,200,000、Indirect Cost: ¥660,000)
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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 / ホスホン酸 / 繊維化阻害 |
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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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Report
(4 results)
Research Products
(26 results)
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[Journal Article] Synthesis of VIP- lipopeptide using a new linker to modify liposomes: towards the development of a drug delivery system for active targeting.2013
Author(s)
Masaka, Toru; Matsuda, Takuya; Li, Yingpeng; Koide, Yuki; Takami, Akira; Yano, Kenji; Imai, Ryosuke; Ichihara, Risa; Yagi, Nobuhiro; Suzuki, Hideharu;
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Journal Title
Chemical & Pharmaceutical Bulletin (2013), 61(11), 1184-1187.
Volume: 61(11)
Pages: 1184-1187
NAID
Related Report
Peer Reviewed
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[Journal Article] N- Benzylation /Benzylic C- H Amidation Cascade by the (η3- Benzyl) palladium System in Aqueous Media: An Effective Pathway for the Direct Construction of 3- Phenyl- 3, 4- dihydro- (2H) - 1, 2, 4- benzothiadiazine 1, 1-Dioxides2013
Author(s)
Hikawa, Hidemasa; Matsuda, Naoya; Suzuki, Hideharu; Yokoyama, Yuusaku; Azumaya, Isao,
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Journal Title
ADVANCED SYNTHESIS & CATALYSIS
Volume: 355(11-12)
Issue: 11-12
Pages: 2308-2320
DOI
Related Report
Peer Reviewed
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[Journal Article] A practical regioselective synthesis of alkylthio- or arylthioindoles without the use of smelly compounds such as thiols.2013
Author(s)
Hamashima, Toshihiko; Mori, Yoshiaki; Sawada, Kazunori; Kasahara, Yuko; Murayama, Daisuke; Kamei, Yuto; Okuno, Hiroaki; Yokoyama, Yuusaku; Suzuki, Hideharu,
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Journal Title
Chemical & Pharmaceutical Bulletin (2013), 61(3), 292-303.
Volume: 61(3)
Pages: 292-303
NAID
Related Report
Peer Reviewed
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[Journal Article] Synthesis and biological evaluation of novel tryptoline derivatives as indoleamine 2, 3- dioxygenase (IDO) inhibitors.2013
Author(s)
Tanaka, Minoru; Li, Xin; Hikawa, Hidemasa; Suzuki, Takafumi; Tsutsumi, Katsuhiko; Sato, Masashi; Takikawa, Osamu; Suzuki, Hideharu; Yokoyama, Yuusaku,
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Journal Title
Bioorganic & Medicinal Chemistry (2013), 21(5), 1159-1165.
Volume: 21(5)
Issue: 5
Pages: 1159-1165
DOI
Related Report
Peer Reviewed
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