Creation of New Lead Compounds using Natural Resources and Metal Nanoparticle Catalysts
Project/Area Number |
22K15252
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Research Category |
Grant-in-Aid for Early-Career Scientists
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Allocation Type | Multi-year Fund |
Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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Research Institution | Osaka University |
Principal Investigator |
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Project Period (FY) |
2022-04-01 – 2024-03-31
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Project Status |
Granted (Fiscal Year 2022)
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Budget Amount *help |
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2023: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Fiscal Year 2022: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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Keywords | natural product extract / metal catalyst / chemical diversification / lead compound |
Outline of Research at the Start |
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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Outline of Annual Research Achievements |
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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Current Status of Research Progress |
Current Status of Research Progress
2: Research has progressed on the whole more than it was originally planned.
Reason
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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Strategy for Future Research Activity |
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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Report
(1 results)
Research Products
(2 results)