Studies of antimicrobial oligosaccharides

2017 Fiscal Year Final Research Report

• Project/Area Number: 15K07857
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Chemical pharmacy
• Research Institution: Nagoya Institute of Technology
• Principal Investigator: Yamamura Hatsuo 名古屋工業大学, 工学(系)研究科(研究院), 教授 (80220440)
• Co-Investigator(Renkei-kenkyūsha): MIYAGAWA Atsushi 名古屋工業大学, 大学院工学研究科, 助教 (60469921)
• Project Period (FY): 2015-10-21 – 2018-03-31
• Keywords: 抗菌 / 抗生物質 / シクロデキストリン / クリック反応

Outline of Final Research Achievements

Novel antibiotics have been highly demanded because of emergence of drug-resistant bacteria. Here we investigated membrane-active antimicrobial oligosaccharide cyclodextrins. These possess functional groups to permeabilize bacterial cell membranes. The polyfunctionalization of sugars was achieved through a microwave-assisted click reaction. A survey using the derivatives with systematically varied functionalities clarified the unique correlation of the antimicrobial activity of these compounds with their structures. The dependence of number of functional groups in the molecule demonstrates that the assembly of the groups is necessary for expressing antimicrobial activity. The compounds having selective toxicity against bacteria including multidrug-resistant pathogens were observed. The results demonstrate that the sugar is a versatile molecular scaffold for rationally designed structures and can be used for the development of new antibiotics.

Free Research Field

有機化学、生物有機化学、シクロデキストリン化学