Synthesis of eudistomin D analogues and its effects on adenosine receptors

2009 Fiscal Year Final Research Report

• Project/Area Number: 20790001
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Chemical pharmacy
• Research Institution: Hokkaido University
• Principal Investigator: ISHIYAMA Haruaki Hokkaido University, 大学院・薬学研究院, 助教 (70333622)
• Project Period (FY): 2008 – 2009
• Keywords: 生薬 / 天然物化学

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.

Research Products

• [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
  • 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
  • Peer Reviewed