Synthesis and structure activity relationship of atpenin A5 derivatives as complex II inhibitors

• Project/Area Number: 21790117
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Single-year Grants
• Research Field: Drug development chemistry
• Research Institution: Kitasato University
• Principal Investigator: OHTAWA Masaki Kitasato University, 薬学部, 助教 (70453503)
• Project Period (FY): 2009 – 2010
• Project Status: Completed (Fiscal Year 2010)
• Budget Amount: ¥2,470,000 (Direct Cost: ¥1,900,000、Indirect Cost: ¥570,000); Fiscal Year 2010: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000); Fiscal Year 2009: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
• Keywords: 天然有機化合物 / 生理活性物質 / 構造活性相関 / 創薬化学 / 天然物

Research Abstract

Comprehensive structure activity relationship of atpenin A5 as a potent complex II inhibitor and the synthesis of atpenin A5/flutolanil chimeric inhibitors has been achieved. On the guidance of this study, we also constructed a potential basis for the discovery of atpenin A5 derivatives as novel antihelminth agents.

Research Products

• [Journal Article] Enantioselective total synthesis of atpenin A5. (2009)
  • Author(s): Ohtawa, M.; Ogihara, S.; Sugiyama, K.; Shiomi, K.; Harigaya, Y.; Nagamitsu, T.; Omura, S.
  • Journal Title: J. Antibiot. 62 Pages: 289-294
  • NAID: 10030635353
  • Peer Reviewed
• [Journal Article] Enantioselective total synthesis of atpenin A5 (2009)
  • Author(s): Ohtawa, M., et. al.
  • Journal Title: The Journal of Antibiotics 62 Pages: 289-294
  • NAID: 10030635353
  • Peer Reviewed
• [Presentation] NFRD阻害剤atpenin類の全合成ならびに構造活性相関研究 (2010)
  • Author(s): 杉山晃平(大多和正樹)
  • Organizer: 日本薬学会第130年会
  • Place of Presentation: 桃太郎アリーナ(岡山)
• [Presentation] Enantioselective total synthesls of atpenins (2009)
  • Author(s): Ohtawa, M., et. al.
  • Organizer: The 11^<th> International Kyoto Conference on New Aspects of Organic Chemistry
  • Place of Presentation: 京都リーガロイヤルホテル(京都府)
  • Year and Date: 2009-11-10
• [Presentation] Fumarate reductase阻害剤atpenin類の全合成ならびに構造活性相関研究 (2009)
  • Author(s): 杉山晃平(大多和正樹)
  • Organizer: 第28回メディシナルケミストリーシンポジウム
  • Place of Presentation: 東京大学安田講堂(東京)
• [Presentation] Enantioselective total synthesis of atpenin A5 and its analogues. (2009)
  • Author(s): 杉山晃平(大多和正樹)
  • Organizer: The 11^<th> International KYOTO conerence on New Aspects of Organic Chemistry.
  • Place of Presentation: リーガロイヤルホテル京都(京都)