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Development of novel antibiotics that inhibit glutamate racemase as transition state analogues

Research Project

Project/Area Number 20790100
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Drug development chemistry
Research InstitutionGifu Pharmaceutical University

Principal Investigator

OKUDA Kensuke  Gifu Pharmaceutical University, 薬学部, 講師 (00311796)

Project Period (FY) 2008 – 2009
Project Status Completed (Fiscal Year 2009)
Budget Amount *help
¥3,770,000 (Direct Cost: ¥2,900,000、Indirect Cost: ¥870,000)
Fiscal Year 2009: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000)
Fiscal Year 2008: ¥3,120,000 (Direct Cost: ¥2,400,000、Indirect Cost: ¥720,000)
Keywords遷移状態類縁体 / フッ素 / 抗菌活性 / グルタミン酸 / 抗生物質
Research Abstract

Emerging and increasing of multidrug resistant bacteria has become an even more serious issue. In this regard, I pointed the aim at glutamate racemase inhibition, which is an essential enzyme for bacteria, as a novel drug target. As human do not have this enzyme, one can expect that inhibitors of this enzyme do not have side effects. I designed and synthesized substrate analogues as potential inhibitors based on their action mechanism. Actually, one compound showed some antimicrobial activity on S. pneumoniae.

Report

(3 results)
  • 2009 Annual Research Report   Final Research Report ( PDF )
  • 2008 Annual Research Report
  • Research Products

    (5 results)

All 2009 Other

All Presentation (3 results) Remarks (2 results)

  • [Presentation] グルタミン酸ラセマーゼ阻害剤を指向する3-フルオロ-D-グルタミン酸の合成2009

    • Author(s)
      河村泰男、植月勇貴、竹内靖雄、上田聡、奥田健介、永澤秀子
    • Organizer
      創薬懇話会2009
    • Place of Presentation
      アルモニーテラッセ(岐阜)
    • Year and Date
      2009-12-10
    • Related Report
      2009 Annual Research Report 2009 Final Research Report
  • [Presentation] グルタミン酸ラセマーゼ阻害剤を指向する3-フルオログルタミン酸の合成2009

    • Author(s)
      河村泰男、植月勇貴、竹内靖雄、上田聡、奥田健介、永澤秀子
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      国立国際京都会館(京都)
    • Year and Date
      2009-03-27
    • Related Report
      2009 Final Research Report
  • [Presentation] グルタミン酸ラセマーゼ阻害剤を指向する3・フルオログルタミン酸の合成2009

    • Author(s)
      河村泰男
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      国立京都国際会館
    • Year and Date
      2009-03-27
    • Related Report
      2008 Annual Research Report
  • [Remarks]

    • URL

      http://www.gifu-pu.ac.jp/research/research_yakka.html

    • Related Report
      2009 Final Research Report
  • [Remarks]

    • URL

      http://www.gifu-pu.ac.jp/research/research_yakka.html

    • Related Report
      2009 Annual Research Report

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Published: 2008-04-01   Modified: 2016-04-21  

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