Development of Antibacterial Natural Products Derivatives

2020 Fiscal Year Final Research Report

• Project/Area Number: 19K16308
• Research Category: Grant-in-Aid for Early-Career Scientists
• Allocation Type: Multi-year Fund
• Review Section: Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
• Research Institution: Hokkaido University
• Principal Investigator: Katsuyama Akira 北海道大学, 薬学研究院, 助教 (20824709)
• Project Period (FY): 2019-04-01 – 2021-03-31
• Keywords: 薬剤耐性菌 / 抗菌薬 / 天然物 / 有機合成化学 / 細胞壁

Outline of Final Research Achievements

A reserch based on natural products with antimicrobial activity was conducted to develop novel antimicrobial agents which are effective against drug-resistant bacteria. We focused on empedopeptin, which is natural product that inhibit bacterial cell wall biosynthesis. Thus, synthetic research of empedopeptin was conducted. We also synthesized lipid II and its related compounds, which are precursors of a bacterial cell wall, to elucidate the mechanism of action of the natural products. As a result, fluorescent probe molecules were synthesized.

Free Research Field

創薬化学

Academic Significance and Societal Importance of the Research Achievements

薬剤耐性菌に対する新規抗菌薬の開発は公衆衛生上の重要な課題である。本研究では薬剤耐性が生じにくい性質に着目した創薬研究により、耐性が生じにくい抗菌薬の創生を目指した。本研究の完遂により、望むような性質を有する抗菌薬が開発できれば、これまでの感染症治療薬において一般的な問題となっていた、薬剤耐性と新薬開発のいたちごっこを脱却できる画期的な新薬の創生が期待できる。