| Budget Amount *help |
¥17,940,000 (Direct Cost: ¥13,800,000、Indirect Cost: ¥4,140,000)
Fiscal Year 2018: ¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2017: ¥6,240,000 (Direct Cost: ¥4,800,000、Indirect Cost: ¥1,440,000)
Fiscal Year 2016: ¥6,630,000 (Direct Cost: ¥5,100,000、Indirect Cost: ¥1,530,000)
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| Outline of Final Research Achievements |
1)Synthesis and biological evaluation of muraimycin analogues were investigated. 2) Synthesis of the core structure of phaerimycin and its derivatives was achieved and their MraY inhibitory activity was also conducted. As a result, one derivative showed high MraY inhibitory activity. 3) Mureidomycin A analigues were synthesized and it was found that some derivatives exhibited higher MraY inhibitory activity and anti-P. aeruginosa activity than pacidamycin D, which is a conger of mureidomycin A. Furthermore, X-ray crystal structure analysis of the complex of mureidomycin analogue bound to MraY was also established. 4) The synthesis and action mechanism analysis of plasbacin A3 and its derivative were conducted. 5) In order to find an effective derivative against colistin resistant bacteria, 30 colistin derivatives were synthesized and their antibacterial activities were evaluated.
Some drug resistant bacterial drug lead were developed in this study.
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