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Elucidation of axial chirality and its application to medicinal chemistry

Research Project

Project/Area Number 21590124
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Drug development chemistry
Research InstitutionTeikyo University

Principal Investigator

NATSUGARI Hideaki  帝京大学, 薬学部, 教授 (00334334)

Co-Investigator(Renkei-kenkyūsha) TABATA Hidetsugu  帝京大学, 薬学部, 助手 (80445634)
Project Period (FY) 2009 – 2011
Project Status Completed (Fiscal Year 2011)
Budget Amount *help
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2011: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2010: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
Fiscal Year 2009: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywords軸不斉 / キラリティー / γ-セクレターゼ阻害薬 / ACAT阻害薬 / バソプレッシン受容体拮抗薬 / ジベンゾジアゼピノン / ベンゾラクタム / 1,5-ベンゾジアゼピノン / 窒素のキラリティー / インドメタシン
Research Abstract

The active conformation of biologically active compounds(e. g.,(1) a γ secretase inhibitor, (2) new vasopressin V_1, V_2 receptor antagonists, and (3) new ACAT inhibitors) was elucidated, and the axial chirality originated from an aryl-amide moiety of the molecules was shown to play important role on exerting the activity.

Report

(4 results)
  • 2011 Annual Research Report   Final Research Report ( PDF )
  • 2010 Annual Research Report
  • 2009 Annual Research Report
  • Research Products

    (37 results)

All 2012 2011 2010 2009 Other

All Journal Article (13 results) (of which Peer Reviewed: 13 results) Presentation (22 results) Book (2 results)

  • [Journal Article] Active conformation of seven-membered-ring benzolactams as new ACAT inhibitors : latent chirality at N5 in the 1, 5-benzodiazepin-2-one nucleus2012

    • Author(s)
      Tabata, Hidetsugu ; Wada, Naoya ; Takada, Yuko ; Nakagomi, Jun ; Miike, Tomohiro ; Shirahase, Hiroaki ; Oshitari, Tetsuta ; Takahashi, Hideyo ; Natsugari, Hideaki
    • Journal Title

      Chemistr-A European Journal

      Volume: 18 Pages: 1572-1576

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Active conformation of seven-membered-ring benzolactams as new ACAT inhibitors: Latent chirality at N5 in the 1,5-benzodiazepin-2-one nucleus2012

    • Author(s)
      Tabata Hidetsugu
    • Journal Title

      Chemistr-A European Journal

      Volume: 18 Issue: 6 Pages: 1572

    • DOI

      10.1002/chem.201103264

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Isolation and characterization of atropisomers of seven-membered-ring benzolactams2011

    • Author(s)
      Tabata, Hidetsugu ; Wada, Naoya ; Takada, Yuko ; Oshitari, Tetsuta ; Takahashi ; Hideyo Natsugari, Hideaki
    • Journal Title

      Journal of Organic Chemistry

      Volume: 76 Pages: 5123-5131

    • Related Report
      2011 Annual Research Report 2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomerism in the vaptan class of vasopressin receptor ligands : the active conformation recognized by the receptor2011

    • Author(s)
      Tabata, Hidetsugu ; Nakagomi, Jun ; Morizono, Daisuke ; Oshitari, Tetsuta ; Takahashi, Hideyo ; Natsugari, Hideaki
    • Journal Title

      Angewandte Chemie International Edition

      Volume: 50 Pages: 3075-3079

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomerism observed in indometacin derivatives2011

    • Author(s)
      Takahashi, Hideyo ; Wakamatsu, Shintaro ; Tabata, Hidetsugu ; Oshitari, Tetsuta ; Harada, Ayako ; Inoue, Keizo, Natsugari, Hideaki
    • Journal Title

      Organic Letters

      Volume: 13 Pages: 760-763

    • Related Report
      2011 Annual Research Report 2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomerism in the vaptan class of vasopressin receptor ligands: The active conformation recognized by the receptor2011

    • Author(s)
      Tabata Hidetsugu
    • Journal Title

      Angewandte Chemie International Edition

      Volume: 50 Issue: 13 Pages: 3075

    • DOI

      10.1002/anie.201007772

    • Related Report
      2011 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomerism Observed in Indometacin Derivatives2011

    • Author(s)
      H.Takahashi, H.Natsugari, et al.
    • Journal Title

      Organic Letters

      Volume: 13 Pages: 760-763

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomerism in the Vaptan Class of Vasopressin Receptor Ligands : the Active Conformation Recognized by the Receptor2011

    • Author(s)
      H.Tabata, H.Natsugari, et al.
    • Journal Title

      Angewandte Chemie Int.Ed.

      Volume: 50 Pages: 3075-3079

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomeric properties of 7-, 8-, and 9-membered-ring dibenzolactams : conformation, thermal stability, and chemical reactivity2010

    • Author(s)
      Tabata, Hidetsugu ; Suzuki, Hiroyuki ; Akiba, Kumi ; Takahashi, Hideyo ; Natsugari, Hideaki
    • Journal Title

      Journal of Organic Chemistry

      Volume: 75 Pages: 5984-5993

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomeric properties of 7-, 8- and 9-membered-ring dibenzolactams : conformation, thermal stability, and chemical reactivity2010

    • Author(s)
      H.Tabata, H.Natsugari, et al.
    • Journal Title

      Journal of Organic Chemistry

      Volume: 75 Pages: 5984-5993

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Chemistry of axial asymmetry. Chemistry associated with receptor-binding study for drug development asymmetry2009

    • Author(s)
      Natsugari, Hideaki
    • Journal Title

      Farumashia

      Volume: 45 Pages: 525-528

    • Related Report
      2011 Final Research Report
    • Peer Reviewed
  • [Journal Article] Dual antitumor mechanisms of Notch signaling inhibitor in a T-cell acute lymphoblastic leukemia xenograft model2009

    • Author(s)
      Masuda Shigeo, et al.
    • Journal Title

      Cancer Science 100

      Pages: 2444-2450

    • Related Report
      2009 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Chemistry of axial asymmetry. Chemistry associated withreceptor-binding study for drug development2009

    • Author(s)
      Natsugari Hideaki
    • Journal Title

      Farumashia 45

      Pages: 525-528

    • Related Report
      2009 Annual Research Report
    • Peer Reviewed
  • [Presentation] Molechular chirality in the vasopressin receptor ligands2011

    • Author(s)
      Jun Nakagomi
    • Organizer
      AIMECS2011
    • Place of Presentation
      京王プラザホテル(東京)
    • Year and Date
      2011-12-01
    • Related Report
      2011 Annual Research Report
  • [Presentation] 7員環ベンゾラクタム類の分子不斉とACAT阻害活性:1,5-ベンゾジアゼピン-2-オンのN5における隠れたキラリティー2011

    • Author(s)
      田畑英嗣
    • Organizer
      第37回反応と合成の進歩シンポジウム
    • Place of Presentation
      あわぎんホール(徳島)
    • Year and Date
      2011-11-08
    • Related Report
      2011 Annual Research Report
  • [Presentation] 7員環ベンゾラクタム類の分子不斉とACAT阻害活性: 1, 5-ベンゾジアゼピン-2-オンにおける5位窒素の隠れたキラリティー2011

    • Author(s)
      田畑英嗣、和田直也、高田裕子、中込純、三池知紘、白波瀬弘明、忍足鉄太、高橋秀依、夏苅英昭
    • Organizer
      第55回日本薬学会関東支部大会
    • Place of Presentation
      千葉
    • Year and Date
      2011-10-08
    • Related Report
      2011 Final Research Report
  • [Presentation] 7員環ベンゾラクタム類の分子不斉とACAT阻害活性:1,5-ベンゾジアゼピン-2-オンにおける5位窒素の隠れたキラリティー2011

    • Author(s)
      田畑英嗣
    • Organizer
      第55回日本薬学会関東支部大会
    • Place of Presentation
      東邦大学薬学部(千葉)
    • Year and Date
      2011-10-08
    • Related Report
      2011 Annual Research Report
  • [Presentation] 7員環ベンゾラクタム類のキラリティー:分子不斉とACAT阻害活性2011

    • Author(s)
      田畑英嗣、和田直也、高田裕子、三池知紘、白波瀬弘明、忍足鉄太、高橋秀依、夏苅英昭
    • Organizer
      第61回有機合成化学協会関東支部大会
    • Place of Presentation
      千葉
    • Year and Date
      2011-05-22
    • Related Report
      2011 Final Research Report
  • [Presentation] 7員環ベンゾラクタム類のキラリティー:分子不斉とACAT阻害活性2011

    • Author(s)
      田畑英嗣
    • Organizer
      第61回有機合成化学協会関東支部大会
    • Place of Presentation
      千葉大学(千葉)
    • Year and Date
      2011-05-22
    • Related Report
      2011 Annual Research Report
  • [Presentation] バソプレシン受容体格抗薬の活性発現に寄与する軸不斉構造2011

    • Author(s)
      中込純
    • Organizer
      シンポジウムモレキュラーキラリティー2011
    • Place of Presentation
      東京工業大学(東京)
    • Year and Date
      2011-05-21
    • Related Report
      2011 Annual Research Report
  • [Presentation] Molecular Chirality in the Vasopressin Receptor Ligands2011

    • Author(s)
      Jun Nakagomi, Hidetsugu Tabata, Daiske Morizono, Tetsuta Oshitari, Hideyo Takahashi, Hideaki Natsugari
    • Organizer
      AIMECS2011
    • Place of Presentation
      Tokyo
    • Related Report
      2011 Final Research Report
  • [Presentation] 7員環ベンゾラクタム類の分子不斉とACAT阻害活性: 1, 5-ベンゾジアゼピン-2-オンのN5における隠れたキラリティー2011

    • Author(s)
      田畑英嗣、和田直也、高田裕子、中込純、忍足鉄太、高橋秀依、三池知紘、白波瀬弘明、夏苅英昭
    • Organizer
      第37回反応と合成の進歩シンポジウム
    • Place of Presentation
      徳島
    • Related Report
      2011 Final Research Report
  • [Presentation] バソプレシン受容体拮抗薬の活性発現に寄与する軸不斉構造2011

    • Author(s)
      中込純、田畑英嗣、森園大輔、忍足鉄太、高橋秀依、夏苅英昭
    • Organizer
      シンポジウムモレキュラー・キラリティー2011
    • Place of Presentation
      東京
    • Related Report
      2011 Final Research Report
  • [Presentation] N-アシルベンゾジアゼピン誘導体の軸性キラリティー2010

    • Author(s)
      中込純、河野晃二、田畑英嗣、忍足鉄太、高橋秀依、夏苅英昭
    • 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
    • Related Report
      2011 Final Research Report
  • [Presentation] 医薬品に秘められたキラリティー-アミド軸不斉の化学-2010

    • Author(s)
      夏苅英昭
    • Organizer
      近畿大学ハイテク・リサーチ・センター整備事業-第9回シンポジウム-
    • Place of Presentation
      近畿大学(大阪)
    • Year and Date
      2010-09-11
    • Related Report
      2010 Annual Research Report
  • [Presentation] 医薬品に秘められたキラリティー-アミド軸不斉の化学-2010

    • Author(s)
      夏苅英昭
    • Organizer
      近畿大学・ハイテク・リサーチ・センター整備業・シンポジウム「有機化学を基盤とする創薬」
    • Place of Presentation
      近畿大学薬学部
    • Year and Date
      2010-09-01
    • Related Report
      2011 Final Research Report
  • [Presentation] ベンゾアゼピノン誘導体の軸性キラリティーとACAT阻害活性-CDスペクトルは絶対配置の決め手になるか-2010

    • Author(s)
      田畑英嗣、和田直也、高田裕子、三池知紘、笠井正恭、白波瀬弘明、忍足鉄太、高橋秀依、夏苅英昭
    • 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
    • Related Report
      2011 Final Research Report
  • [Presentation] 7/8/9員環ジベンゾラクタム類の軸性キラリティーと立体化学2010

    • Author(s)
      田畑英嗣、鈴木啓志、高橋秀依、夏苅英昭
    • Organizer
      第40回複素環化学討論会
    • Place of Presentation
      仙台
    • Related Report
      2011 Final Research Report
  • [Presentation] 軸性キラリティーを有するビフェニルラクタム類の立体化学の解明2010

    • Author(s)
      田畑英嗣、鈴木啓志、高橋秀依、夏苅英昭
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Related Report
      2011 Final Research Report
  • [Presentation] 2H-1, 5-ベンゾジアゼピン-2-オン誘導体の合成とその立体化学2010

    • Author(s)
      和田直也、田畑英嗣、高橋秀依、夏苅英昭
    • Organizer
      日本薬学会第129年会
    • Place of Presentation
      京都
    • Related Report
      2011 Final Research Report
  • [Presentation] 医薬品に秘められたキラリティー2009

    • Author(s)
      夏苅英昭
    • Organizer
      第37回構造活性相関シンポジウム
    • Place of Presentation
      北里大学薬学部
    • Year and Date
      2009-11-12
    • Related Report
      2011 Final Research Report
  • [Presentation] 医薬品に秘められたキラリティー2009

    • Author(s)
      夏苅英昭
    • Organizer
      第37回構造活性相関シンポジウム
    • Place of Presentation
      北里大学・薬学部
    • Year and Date
      2009-11-12
    • Related Report
      2009 Annual Research Report
  • [Presentation] ビフェニルラクタム類の軸性キラリティーの解明2009

    • Author(s)
      田畑英嗣、鈴木啓志、高橋秀依、夏苅英昭
    • Organizer
      第53回日本薬学会関東支部大会
    • Place of Presentation
      東京
    • Year and Date
      2009-10-03
    • Related Report
      2011 Final Research Report
  • [Presentation] ジベンゾ[b, d]アゼピン-6-オン誘導体の軸性キラリティーと立体化学2009

    • Author(s)
      田畑英嗣、高橋秀依、夏苅英昭
    • Organizer
      第57回有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      東京
    • Related Report
      2011 Final Research Report
  • [Presentation] N-アシルベンゾジアゼピン誘導体の軸性キラリティーと生物活性

    • Author(s)
      田畑英嗣、和田直也、高田裕子、三池知紘、笠井正恭、白波瀬弘明、忍足鉄太、高橋秀依、夏苅英昭
    • Organizer
      日本薬学会第131年会
    • Place of Presentation
      静岡
    • Related Report
      2011 Final Research Report
  • [Book] スタンダード薬学シリーズ3・化学系薬学I(第二版)2010

    • Author(s)
      夏苅英昭
    • Publisher
      東京化学同人
    • Related Report
      2011 Final Research Report
  • [Book] スタンダード薬学シリーズ3・化学系薬学I(第二版)2010

    • Author(s)
      夏苅英昭(共編・共著)
    • Total Pages
      361
    • Publisher
      東京化学同人
    • Related Report
      2009 Annual Research Report

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Published: 2009-04-01   Modified: 2016-04-21  

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