2013 Fiscal Year Final Research Report
Structure- activity relationship study of nafuredin-gamma derivatives as complex I selective inhibitors
| Project/Area Number |
23590132
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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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| Research Field |
Drug development chemistry
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| Research Institution | Kitasato University |
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Principal Investigator |
ARIMA Shiho 北里大学, 薬学部, 助教 (20276158)
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| Project Period (FY) |
2011 – 2013
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| Keywords | 医薬品化学 / 構造活性相関 |
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| Research Abstract |
Nafuredin-gamma, converted from nafuredin as a fungal metabolite under mild basic conditions, demonstrates inhibitory activity and selectivity against complex I of Ascaris suum. These compounds have unique and useful biological activities; however, the conjugated diene moieties included in the structure are highly unstable in the presence of oxygen. To solved this problem, stable nafuredin-gamma derivatives with non-conjugated (E)-olefins in the side chain moiety designed and synthesized. These derivatives showed moderate complex I inhibitory activities and high stabilities in air .
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