2017 Fiscal Year Final Research Report
Toward the total synthesis of novel anti-protozoal 12-membered macrolides
| Project/Area Number |
15K07866
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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 |
Chemical pharmacy
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| Research Institution | Kitasato University |
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Principal Investigator |
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| Project Period (FY) |
2015-04-01 – 2018-03-31
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| Keywords | 全合成 / アクチノアロライド / マクロライド / トリパノソーマ / 新規天然物 |
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| Outline of Final Research Achievements |
Trypanosomiasis is caused by the parasitic flagellated protozoa. During the course of physicochemical screening for metabolites, new anti-trypanosomal macrolides, actinoallolides, were discovered. Among them, actinoallolide A showed most potent and selective anti-trypanosomal activity. Due to its intriguing architectural structure and interesting biological activity, we thus became interested to determination of their absolute and total synthesis of actinoallorides.
We first determined the absolute configuration of actinoalloride A by single-crystal X-ray crystallographic analysis of its acylation derivative. We next commenced to pursue the synthetic studies of actinoalloride A to provide clarification of detailed structure-activity relationships. So far, we have achieved the synthesis of an essential intermediate including full carbon framework in the total synthesis of Actinoallolide A.
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| Free Research Field |
天然物合成化学
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