Development of novel antifungal based on chemical synthesis
| Project/Area Number |
15K13645
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| Research Category |
Grant-in-Aid for Challenging Exploratory Research
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| Allocation Type | Multi-year Fund |
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| Research Field |
Organic chemistry
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| Research Institution | Kyushu University |
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Principal Investigator |
Oishi Tohru 九州大学, 理学研究院, 教授 (90241520)
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| Co-Investigator(Renkei-kenkyūsha) |
EBINE Makoto 九州大学, 大学院理学研究院, 助教 (70545574)
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| Research Collaborator |
TAKADA Yuri
WAKAMIYA Yuma
YANAI Naoto
KOGE Tomoyuki
KATAYAMA Sota
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| Project Period (FY) |
2015-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2015: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
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| Keywords | アンフィジノール３ / 天然物 / 抗真菌物質 / ポリエンポリオール化合物 / 化学合成 |
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| Outline of Final Research Achievements |
The fluorescent molecular probe possessing the C43-C67 part of amphidinol 3 (AM3) was synthesized. Although liposomes were incubated with the molecular probe and observed by using fluorescence microscope, no fluorescent was detected. These results suggested that the C43-C67 part of AM3 was not enough to interact with lipid membrane and useful information to design new molecule possessing high affinity with lipid membranes.
As a part of the structure-activity relationship studies to elucidate structure requirements for eliciting antifungal activity, a truncated analog corresponding to the C21-C39/C52-C67 section of AM3 was synthesized by using Suzuki-Miyaura coupling and Julia-Kocienski olefination as key steps. Although the biological activity of the analog was evaluated, it elicited no antifungal activity. These results that the two tetrahydropyran rings of AM3 are necessary to elicit antifungal activity.
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Report
(3 results)
Research Products
(21 results)
