2020 Fiscal Year Final Research Report
Development of resolvin analogues as a metabolically stable equivalent
| Project/Area Number |
19K16307
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| Research Category |
Grant-in-Aid for Early-Career Scientists
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| Allocation Type | Multi-year Fund |
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| Review Section |
Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
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| Research Institution | Hokkaido University |
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Principal Investigator |
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| Project Period (FY) |
2019-04-01 – 2021-03-31
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| Keywords | レゾルビン / ω-3系脂肪酸 / 代謝安定化 |
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| Outline of Final Research Achievements |
We have designed resolvin E1 and E2 analogues substituted omega-terminal to develop a metabolically stable equivalent. In order to synthesize them efficiently, we planned that resolvin E1 and E2 were separated into three fragments and connected them respectively. As a result, we achieved the synthesis of three fragments and connected them by selective olefination. This synthetic route allowed to introduce omega-terminal moiety at the late stage.
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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 |
レゾルビン類はその強力な抗炎症作用から新規抗炎症薬のリード構造として注目されているが、生体内で容易に代謝されて分解・不活性化されてしまうことが知られている。この不安定性が影響し、作用機序の解明や構造活性相関研究が進んでいない。このため、誘導体化による安定化や構造活性相関研究が望まれている。本研究で確立した合成経路はこの問題解決のための糸口となり、レゾルビンを基盤とした新規抗炎症薬創出へと発展が期待される。
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