Synthetic chemistry for the development of oligosaccharide-type sialidase inhibitors
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- Hirai Go
- Principal Investigator
- 九州大学
About this project
- Japan Grant Number
- JP18H02097
- Funding Program
- Grants-in-Aid for Scientific Research
- Funding organization
- Japan Society for the Promotion of Science
- Project/Area Number
- 18H02097
- Research Category
- Grant-in-Aid for Scientific Research (B)
- Allocation Type
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- Single-year Grants
- Review Section / Research Field
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- Basic Section 37020:Chemistry and chemical methodology of biomolecules-related
- Research Institution
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- Kyushu University
- Project Period (FY)
- 2018-04-01 〜 2022-03-31
- Project Status
- Completed
- Budget Amount*help
- 16,770,000 Yen (Direct Cost: 12,900,000 Yen Indirect Cost: 3,870,000 Yen)
Research Abstract
We have found that novel disaccharide analogues are effective inhibitors of sialidase despite their substrate structure. Conversion to oligosaccharide structure from these analogs is expected to be a more effective inhibitors for sialidases. Therefore, in this study, we worked to establish an efficient synthetic method. Although we could not achieve the site-selective C-H insertion reaction at the C3 position, we succeeded in introducing acetic acid or malonic acid units by oxidative radical coupling, and achieved the modification of C3-position of the sialic acid in only four steps. Furthermore, the results suggest that this route may also improve the efficiency of glycosylation, which was another problem.
Details 詳細情報について
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- CRID
- 1040000781993026432
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- Text Lang
- ja
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- Data Source
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- KAKEN