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2019 Fiscal Year Final Research Report

Convergent Total Synthesis of Efrotomycin, a Potent Antianaerobic Product

Research Project

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Project/Area Number 19K21230
Project/Area Number (Other) 18H06112 (2018)
Research Category

Grant-in-Aid for Research Activity Start-up

Allocation TypeMulti-year Fund (2019)
Single-year Grants (2018)
Review Section 0801:Pharmaceutical sciences and related fields
Research InstitutionKitasato University

Principal Investigator

Ikeda Akari  北里大学, 感染制御科学府, 特任助教 (40825056)

Project Period (FY) 2018-08-24 – 2020-03-31
Keywords全合成 / エフロトマイシン / efrotomycin / C.difficile感染症 / 収束的 / 嫌気性菌 / 鎖状天然物
Outline of Final Research Achievements

Clostridium difficile (CD) is anaerobic bacteria that cause a more severe form of antibiotic associated diarrhea. However, only a few pharmaceuticals are effective against the bacteria. During the course of screening for metabolites, Efrotomycin was discovered as an anti-CD lead compound. Due to its selective and high activity for CD, we thus became interested to total synthesis of Efrotomycin.
We planned a convergent synthesis of Efrotomycin to provide clarification of detailed structure-activity relationships. So far, we have achieved the convenience method for constructing three-substituted olefin as a key structure, and synthesis of an essential intermediate in the total synthesis of efrotomycin.

Free Research Field

天然物合成化学

Academic Significance and Societal Importance of the Research Achievements

エフロトマイシンの合成報告は1例あるが、その全合成経路は直線的であり、創薬研究に必要な類縁体の合成検討は難しい。本研究ではこの困難さを克服すべく、エフロトマイシンを4つの部分骨格に分割し、うち2つの骨格に共通する3置換オレフィン構造の効率的な構築法を確立することで、大幅な反応の効率化を実現した。これにより本全合成が達成された際には、エフロトマイシンの多様な類縁体を効率良く構築できる点において学術的な意義を有する。
さらに本研究は、抗菌活性に着目した研究に貢献できることからも、抗C.difficile活性を有する化合物の創薬研究として大きな社会的意義を持つ。

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Published: 2021-02-19  

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