2023 Fiscal Year Final Research Report
Optimization of SARS 3CL protease inhibitor and development of anti-COVID-19 drug
| Project/Area Number |
21K05417
|
|---|
| Research Category |
Grant-in-Aid for Scientific Research (C)
|
| Allocation Type | Multi-year Fund |
|---|
| Section | 一般 |
|---|
| Review Section |
Basic Section 38040:Bioorganic chemistry-related
|
|---|
| Research Institution | Kyoto Pharmaceutical University |
|---|
Principal Investigator |
|
|---|
| Co-Investigator(Kenkyū-buntansha) |
今野 博行 山形大学, 大学院理工学研究科, 教授 (50325247)
|
|---|
| Project Period (FY) |
2021-04-01 – 2024-03-31
|
| Keywords | COVID-19 / SARS 3CLプロテアーゼ / 阻害剤 / デカヒドロイソキノリン |
|---|
| Outline of Final Research Achievements |
We demonstrated design and synthesis of decahydroisoquinoline type SARS 3CL protease inhibitors to develop a therapeutic agent for COVID-19. We designed three types of inhibitors and completed the synthesis of the inhibitor precursor for two types. For another type of inhibitor, we performed the conditions for adding the functional group, which introduces the substituent to interact with the protease. We succeeded in improving the yield and confirmed that the functional group was introduced with high stereoselectivity.
|
| Free Research Field |
生物有機化学
|
| Academic Significance and Societal Importance of the Research Achievements |
現在、COVID-19治療薬は存在するが、制限もあり課題もある。COVID-19の原因ウイルスであるSARS-CoV-2は増殖にSARS 3CLプロテアーゼを必須とすることから、本酵素の阻害剤は有望な抗COVID-19薬の標的となりうる。本研究では３種類の阻害剤候補化合物の設計と合成を行い、既存の治療薬や阻害剤と異なる骨格を有する化合物の合成がほぼ完了した。これまでの研究より、本化合物は阻害活性を有すると考えられることから、構造活性相関研究の前向きな進展を期待できる。
|
