| Budget Amount *help |
¥45,500,000 (Direct Cost: ¥35,000,000、Indirect Cost: ¥10,500,000)
Fiscal Year 2019: ¥8,840,000 (Direct Cost: ¥6,800,000、Indirect Cost: ¥2,040,000)
Fiscal Year 2018: ¥8,840,000 (Direct Cost: ¥6,800,000、Indirect Cost: ¥2,040,000)
Fiscal Year 2017: ¥8,840,000 (Direct Cost: ¥6,800,000、Indirect Cost: ¥2,040,000)
Fiscal Year 2016: ¥8,840,000 (Direct Cost: ¥6,800,000、Indirect Cost: ¥2,040,000)
Fiscal Year 2015: ¥10,140,000 (Direct Cost: ¥7,800,000、Indirect Cost: ¥2,340,000)
|
|---|
| Outline of Final Research Achievements |
We have developed a method for efficiently synthesizing cyclic peptide natural products and their analogues exhibiting biological activities. Their three-dimensional structures were clarified by X-ray crystal structure analysis and/or a distance geometry method based on NMR studies. We found that it is important to consider the membrane permeability of the cyclic peptides. Generally, cyclic peptides have a large polar surface area and low membrane permeability. In cyclic peptides that exhibit biological activity, however, the polar surface area decreases due to the intramolecular hydrogen bond between the amide bonds, resulting in sufficient membrane permeability. In addition, we have developed an asymmetric aldol reaction and Mannich reaction utilizing a flow system and have realized reaction integration that can efficiently supply starting materials required for the synthesis of middle-size molecules.
|
