| Project/Area Number |
20590114
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Drug development chemistry
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| Research Institution | Matsuyama University |
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Principal Investigator |
KAWASE Masami Matsuyama University, 薬学部, 教授 (20112641)
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| Co-Investigator(Kenkyū-buntansha) |
HAGIMOTO Yuri 松山大学, 薬学部, 講師 (30435078)
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| Co-Investigator(Renkei-kenkyūsha) |
SAKAGAMI Hiroshi 明海大学, 歯学部, 教授 (50138484)
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| Project Period (FY) |
2008 – 2010
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| Project Status |
Completed (Fiscal Year 2010)
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| Budget Amount *help |
¥4,550,000 (Direct Cost: ¥3,500,000、Indirect Cost: ¥1,050,000)
Fiscal Year 2010: ¥780,000 (Direct Cost: ¥600,000、Indirect Cost: ¥180,000)
Fiscal Year 2009: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2008: ¥2,860,000 (Direct Cost: ¥2,200,000、Indirect Cost: ¥660,000)
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| Keywords | 化合物ライブラリー / カルボニル化合物 / トリフルオロメチルケトン / クロロジフルオロメチルケトン / ヒドロキシケトン / アポトーシス / オートファジー / クオラムセンシング / トリフルオロメチル / ピロール / クロロジフルオロメチルケト / ジフルオロメチルケトン / 抗菌活性 / 構造活性相関 / Dakin-West反応 / N-チオアシルプロリン / 活性型カルボニル / テトラハイドロイソキノリ / 細胞毒性 / ジフルオロクロロメチルケ / N-アシルプロリン / 口腔癌 |
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| Research Abstract |
A novel transformation of N-acylprolines to enol esters was realized by utilizing chlorodifluoroacetic or trifluoroacetic anhydrides in the presence of inorganic bases. Mesoionic 4-trifluoroacetyl-1,3-oxazolium-5-olates reacted with phosphorus-ylides to give 3(beta)-trifluoromethylpyrroles in good yields. Biological results : Screenings of a variety of structurally diverse ketones led to the identification of several apoptosis- and autophagy-inducers and quorum sensing (QS) inhibitors of alpha-trifluoromethylacyloins, N-acyl-1,2,3,4-tetrahydroisoquinolines, and 2-trifluoroacetonylbenzoxazoles as a lead molecule.
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