Multifaceted approaches to develop novel antibacterial seeds against drug-resistant bacterial pathogens

2015 Fiscal Year Final Research Report

• Project/Area Number: 25293026
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Partial Multi-year Fund
• Section: 一般
• Research Field: Drug development chemistry
• Research Institution: Hokkaido University
• Principal Investigator: ICHIKAWA Satoshi 北海道大学, 薬学研究科(研究院), 教授 (60333621)
• Project Period (FY): 2013-04-01 – 2016-03-31
• Keywords: 天然物 / 抗菌剤 / 有機合成

Outline of Final Research Achievements

a) Structural simplification of muraymycins and caprazamycins have been investigated to develop analogues possessing antibacterial activity against drug-resistant bacteria such as MRSA and VRE with enough metabolic stability as well as reduced toxicity against human cells. b) Efficient synthetic strategy toward the synthesis of plusbacin A3, which is applicable to the synthesis of a range of analogues, has been developed. c) Total synthesis of quinaldopeptin has been developed via solid-phase synthesis. A range of analogues was synthesized and their antibacterial activity was evaluated to find a potent analogue with superior antibacterial activity than that of natural product.

Free Research Field

創薬化学