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Synthesis of eudistomin D analogues and its effects on adenosine receptors

Research Project

Project/Area Number 20790001
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Chemical pharmacy
Research InstitutionHokkaido University

Principal Investigator

ISHIYAMA Haruaki  Hokkaido University, 大学院・薬学研究院, 助教 (70333622)

Project Period (FY) 2008 – 2009
Project Status Completed (Fiscal Year 2009)
Budget Amount *help
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2009: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2008: ¥2,730,000 (Direct Cost: ¥2,100,000、Indirect Cost: ¥630,000)
Keywords生薬 / 天然物化学 / カフェイン / アデノシン受容体 / ハイブリッド化合物
Research Abstract

Two analogues of eudistomin D, a β-carboline alkaloid from a marine tunicate Eudistoma olivaceum, were synthesized, and their affinity and selectivity for adenosine receptor subtypes A_1, A_<2A>, and A_<3> were examined. Both compounds exhibited the moderate affinity to the receptor A_3. On the other hand, four bis-N-n-propyl analogues in the uracil ring of two hybridmolecules of caffeine and eudistomin D were synthesized, and their affinity and selectivity for adenosinereceptors A1, A_<2A>, and A_3 were examined. One of the compounds showed the most potent affinity foradenosine receptor A_3 subtype.

Report

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

    (4 results)

All 2009 2008

All Journal Article (4 results) (of which Peer Reviewed: 4 results)

  • [Journal Article] Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors Bioorg.2009

    • Author(s)
      Ishiyama, H.; Nakajima, H.; Nakata, H.; Kobayashi, J.
    • Journal Title

      Med. Chem. 17

      Pages: 4280-4284

    • Related Report
      2009 Final Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors2009

    • Author(s)
      Ishiyama, H.
    • Journal Title

      Bioorg.Med.Chem. 13

      Pages: 4280-4284

    • Related Report
      2009 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis of eudistomin D analogues and its effects on adenosine receptors Bioorg.2008

    • Author(s)
      Ishiyama, H.; Ohshita, K.; Abe, T.; Nakata, H.; Kobayashi, J.
    • Journal Title

      Med. Chem. 16

      Pages: 3825-3830

    • Related Report
      2009 Final Research Report
    • Peer Reviewed
  • [Journal Article] Synthesis of eudistomin D analogues and its effects on adenosine receptors2008

    • Author(s)
      Ishiyama, H
    • Journal Title

      Bioorg. Med. Chem 16

      Pages: 3825-3830

    • Related Report
      2008 Annual Research Report
    • Peer Reviewed

URL: 

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

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