2022 Fiscal Year Final Research Report
Development of convergent synthtic strategy for novel polycyclic exhibiting inhibit activity for 11b-HSD1
| Project/Area Number |
20K06949
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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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| Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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| Research Institution | Tokyo University of Pharmacy and Life Science |
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Principal Investigator |
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| Project Period (FY) |
2020-04-01 – 2023-03-31
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| Keywords | 有機合成化学 / メロテルペノイド / マンギノイド |
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| Outline of Final Research Achievements |
In 2017, manginoids, which are novel polycyclic meroterpenoids containing a spiro ring, were isolated and revealed to have 11β-HSD1 inhibitory activity. Therefore, with the aim of providing samples for more detailed biological activity tests of manginoids and creating compounds with better activity than natural products, we are conducting research with the aim of establishing a convergent synthetic route that can be adapted to derivative synthesis. As a result, we succeeded in establishing a method for constructing tricyclic compounds containing a spiro ring, which is the key skeleton of manginoids. Next, using this established synthetic route, we expanded our research into the synthesis of manginoid E, which has the most complicated structure among manginoids, and were one step closer to establishing a skeleton construction method.
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| Free Research Field |
有機合成化学
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| Academic Significance and Societal Importance of the Research Achievements |
マンギノイド類は11β-HSD1阻害活性を有する多環式メロテルペノイドである。11β-HSD1阻害剤は二型糖尿病などの生活習慣病に対する治療薬として注目されている化合物である。本研究の研究成果は、これまでにない新規骨格の構築法の確立という学術的意義および新たな生活習慣病治療薬のシード化合物創出という社会的意義を有する。
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