研究課題/領域番号 |
22K15252
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研究種目 |
若手研究
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配分区分 | 基金 |
審査区分 |
小区分47010:薬系化学および創薬科学関連
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研究機関 | 大阪大学 |
研究代表者 |
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研究期間 (年度) |
2022-04-01 – 2024-03-31
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研究課題ステータス |
交付 (2022年度)
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配分額 *注記 |
4,680千円 (直接経費: 3,600千円、間接経費: 1,080千円)
2023年度: 2,340千円 (直接経費: 1,800千円、間接経費: 540千円)
2022年度: 2,340千円 (直接経費: 1,800千円、間接経費: 540千円)
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キーワード | natural product extract / metal catalyst / chemical diversification / lead compound |
研究開始時の研究の概要 |
Natural products (NPs) play invaluable roles for drug discovery and development. However, during last two decades, the de-emphasis of NP research correlated to overall reduction in new leads and drug approval. To create brand new biologically active compounds from NPs, we set up our methodology by using of diversity-oriented synthesis of NP extracts, via metal nanoparticle catalysts. This synthesis could directly access a number of NP-like compounds in one-step. Our new approach is promising for faster and more efficient drug discovery and development.
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研究実績の概要 |
We accomplished to discover unprecedented chemical conversion and produce a new compound through a one-step reaction of substances present in the extract of marine sponge Petrosia (Strongylophora) sp. Chemical diversification of the substances present in the natural product extract with heat-treated EtOH produced a new, unexpected tetracyclic bromopyrrole-imidazole derivative, rac-6-OEt-cylindradine A. We also confirmed that it originated from naturally occurring (-)-cylindradine A via a new reaction pattern. Moreover, (-)-dibromophakellin and 4,5-dibromopyrrole-2-carboxylic acid as well as (-)-cylindradine A were reported herein for the first time in this genus. Studies on the possible reaction mechanism and bioactivities were also conducted. The results indicate that the direct chemical diversification of substances present in natural product extracts can be a speedy and useful strategy for the discovery of new compounds.
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現在までの達成度 (区分) |
現在までの達成度 (区分)
2: おおむね順調に進展している
理由
Based on our previous successful study of direct chemical diversification of substances present in natural product extracts, we're trying to apply this method to natural sources using Pd nanoparticle catalyst. Using metal nanoparticle catalyst can efficiently catalyze C-H bond activation, C-C cleavage, and/or cross-coupling to give other scaffolds via C-C and/or C-heteroatom bond formation. Higher reactive Rh nanoparticle catalyst is in developing process.
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今後の研究の推進方策 |
The purpose of this research is to develop a new methodology for creating and discovering new biologically active compounds using natural resources and highly reactive metal nanoparticle catalysts. We're going to apply this methodology to natural sources using various metal nanoparticle catalysts, such as Pd and Rh. This synthesis which could directly access a number of NP-like compounds in one-step is promising for faster and more efficient drug discovery and development.
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