2022 Fiscal Year Research-status Report
Creation of New Lead Compounds using Natural Resources and Metal Nanoparticle Catalysts
| Project/Area Number |
22K15252
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| Research Institution | Osaka University |
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Principal Investigator |
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| Project Period (FY) |
2022-04-01 – 2024-03-31
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| Keywords | natural product extract / metal catalyst / chemical diversification / lead compound |
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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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| Causes of Carryover |
Due to the covid-19 epidemic, ordering and shipping of some chemical reagents were delayed.
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Research Products
(2 results)
