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2012 Fiscal Year Final Research Report

Total synthesis and structure-activity relationship study of pyripyropene A, a potent and selective ACAT2 Inhibitor

Research Project

  • PDF
Project/Area Number 22590011
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Chemical pharmacy
Research InstitutionKitasato University

Principal Investigator

NAGAMITSU Tohru  北里大学, 薬学部, 教授 (90300756)

Project Period (FY) 2010 – 2012
Keywords合成化学 / 創薬化学
Research Abstract

We have achieved a stereocontrolled total synthesis of pyripyropene A (1), a potent ACAT2 inhibitor with high isozyme selectivity. Extension of this chemistry for the structure-activity relationship study successfully produced new A-ring truncated pyripyropene A analogs.

  • Research Products

    (22 results)

All 2013 2012 2011 2010 Other

All Journal Article (1 results) (of which Peer Reviewed: 1 results) Presentation (17 results) Remarks (1 results) Patent(Industrial Property Rights) (3 results)

  • [Journal Article] Total Synthesis of Pyripyropene A2011

    • Author(s)
      Odani, A.; Ishihara, K.; Ohtawa, M.; Tomoda, H.; Omura, S.; Nagamitsu, T
    • Journal Title

      Tetrahedron

      Volume: Vol. 67, No. 42 Pages: 8159-8203

    • URL

      http://dx.doi.org/10.1016/j.tet.2011.06.084

    • Peer Reviewed
  • [Presentation] ACAT2 選択的阻害剤pyripyropene A構造簡略型誘導体の合成研究2013

    • Author(s)
      寺山富明
    • Organizer
      日本薬学会第133年会
    • Place of Presentation
      横浜
    • Year and Date
      2013-03-29
  • [Presentation] ACAT2選択的阻害剤pyripyropene Aの全合成および創薬研究2012

    • Author(s)
      大多和正樹
    • Organizer
      第30回白金シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2012-12-18
  • [Presentation] Structure-activity relationship of new pyripyropene A derivatives, inhibitors of acyl-CoA:cholesterol acyltranferase 22012

    • Author(s)
      Ohtawa M
    • Organizer
      13th Tetrahedron Symposium - Asia Edition
    • Place of Presentation
      Taipei, Taiwan
    • Year and Date
      2012-11-28
  • [Presentation] Total synthesis of pyripyropene A2012

    • Author(s)
      Nagamitsu T
    • Organizer
      13th Tetrahedron Symposium - Asia Edition
    • Place of Presentation
      Taipei, Taiwan
    • Year and Date
      2012-11-28
  • [Presentation] ACAT2 選択的阻害剤pyripyropene Aの形式全合成2011

    • Author(s)
      石原雅織
    • Organizer
      AKPS集会第7回北里化学シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2011-12-22
  • [Presentation] Pyripyropene Aの低分子化誘導体の合成研究2011

    • Author(s)
      寺山富明
    • Organizer
      AKPS集会 第7回北里化学シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2011-12-22
  • [Presentation] Stracture-activity relationship of new pyripyropene A derivatives, inhibitors of acyl-CoA:cholesterole acyltransferase 2, AIMECS II2011

    • Author(s)
      Ohtawa, M
    • Organizer
      The 8th AFMC International Medicinal Chemistry Symposium
    • Place of Presentation
      Tokyo
    • Year and Date
      2011-12-01
  • [Presentation] ACAT2選択的阻害剤pyripyropen Aの構造活性相関ならびに全合成2011

    • Author(s)
      大多和正樹
    • Organizer
      第53回天然有機化合物討論会
    • Place of Presentation
      大阪
    • Year and Date
      2011-09-27
  • [Presentation] ACAT2 選択的阻害剤pyripyropene Aの形式全合成2011

    • Author(s)
      小谷篤輝
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Year and Date
      2011-03-30
  • [Presentation] Pyripyropene Aの新規低分子誘導体の合成研究2011

    • Author(s)
      市田直樹
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Year and Date
      2011-03-30
  • [Presentation] ACAT2 選択的阻害剤pyripyropene Aの形式全合成2010

    • Author(s)
      小谷篤輝
    • Organizer
      第60回有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      新潟
    • Year and Date
      2010-12-05
  • [Presentation] Pyripyropene Aの新規低分子誘導体の合成研究2010

    • Author(s)
      市田直樹
    • Organizer
      第29回メディシナルケミストリーシンポジウム
    • Place of Presentation
      京都
    • Year and Date
      2010-11-17
  • [Presentation] ACAT2 選択的阻害剤pyripyropene Aの形式全合成2010

    • Author(s)
      小谷篤輝
    • Organizer
      第29回メディシナルケミストリーシンポジウム
    • Place of Presentation
      京都
    • Year and Date
      2010-11-17
  • [Presentation] ACAT2 選択的阻害剤pyripyropene Aの形式全合成2010

    • Author(s)
      小谷篤輝
    • Organizer
      54回日本薬学会関東支部大会
    • Place of Presentation
      東京
    • Year and Date
      2010-10-02
  • [Presentation] Pyripyropene Aの新規低分子誘導体の合成研究2010

    • Author(s)
      市田直樹
    • Organizer
      第54回日本薬学会関東支部大会
    • Place of Presentation
      東京
    • Year and Date
      2010-10-02
  • [Presentation] ACAT2 選択的阻害剤pyripyropene Aの誘導体合成と構造活性相関2010

    • Author(s)
      大多和正樹
    • Organizer
      第5回医薬品原料国際展 医薬品化学研究発表大会 アカデミックシンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2010-06-30
  • [Presentation] Structure-activity relationship of new pyripyropene A derivatives, inhibitors of acyl-CoA:cholesterol acyltransferase 22010

    • Author(s)
      Ohtawa M
    • Organizer
      The 21st French-Japanese Symposium on Medicinal and Fine Chemistry
    • Place of Presentation
      Kyoto
    • Year and Date
      2010-05-10
  • [Remarks]

    • URL

      http://www.pharm.kitasato-u.ac.jp/orgsynth/saito/TOP_PAGE.html

  • [Patent(Industrial Property Rights)] ACAT2阻害活性を示すピリピロペンA構造簡略型誘導体2013

    • Inventor(s)
      大多和正樹、大村智、供田洋、長光亨
    • Industrial Property Rights Holder
      大多和正樹、大村智、供田洋、長光亨
    • Industrial Property Number
      特願 2013-012868
    • Filing Date
      2013-01-28
  • [Patent(Industrial Property Rights)] ACAT2阻害活性を示す代謝酵素に安定なピリピロペン誘導体2011

    • Inventor(s)
      供田洋、長光亨、松田大介、大城太一、大多和正樹、大村智
    • Industrial Property Rights Holder
      供田洋、長光亨、松田大介、大城太一、大多和正樹、大村智
    • Industrial Property Number
      PCT/2011/057336
    • Filing Date
      2011-03-25
  • [Patent(Industrial Property Rights)] ACAT2阻害活性を示す水酸基含有ピリピロペン誘導体2010

    • Inventor(s)
      供田洋、長光亨、松田大介、大城太一、大多和正樹、大村智
    • Industrial Property Rights Holder
      供田洋、長光亨、松田大介、大城太一、大多和正樹、大村智
    • Industrial Property Number
      PCT/2010/060461
    • Filing Date
      2010-06-21

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Published: 2014-08-29  

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