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Design, Synthesis, and Structure-Activity Relationship Study of Novel Neuro-Protecting Drugs Based on Natural Product Hybridization

Research Project

Project/Area Number 25460010
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Research Field Chemical pharmacy
Research InstitutionUniversity of Toyama

Principal Investigator

Matsuya Yuji  富山大学, 大学院医学薬学研究部(薬学), 教授 (50255858)

Co-Investigator(Renkei-kenkyūsha) SUGIMOTO KENJI  富山大学, 大学院医学薬学研究部, 准教授 (60400264)
TOHDA CHIHIRO  富山大学, 和漢医薬学総合研究所, 准教授 (10272931)
Project Period (FY) 2013-04-01 – 2016-03-31
Project Status Completed (Fiscal Year 2015)
Budget Amount *help
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2015: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2014: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2013: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywordsハイブリッド化 / 天然物 / 神経賦活作用 / カップリング反応 / ハブリッド化 / デノソミン
Outline of Final Research Achievements

Novel hybridization compounds between steroidal natural product "denosomin" and its potential molecular target receptor "vitamin D3" were designed for the purpose of development of novel neuro-protecting agent toward Alzheimer disease chemotherapy. The syntheses were achieved by means of convergent synthetic strategy using palladium-catalyzed coupling reactions. The synthesized hybrid compounds were subjected to assay for their neuro-protecting activity, and new derivatives showing more potent activity than positive control compound "denosomin" were discovered.

Report

(4 results)
  • 2015 Annual Research Report   Final Research Report ( PDF )
  • 2014 Research-status Report
  • 2013 Research-status Report
  • Research Products

    (7 results)

All 2016 2015 2014 2013

All Journal Article (1 results) (of which Peer Reviewed: 1 results,  Open Access: 1 results,  Acknowledgement Compliant: 1 results) Presentation (6 results) (of which Int'l Joint Research: 1 results,  Invited: 2 results)

  • [Journal Article] Synthesis of Denosomin-Vitamin D3 Hybrids and Evaluation of their Anti-Alzheimer’s Disease Activities.2015

    • Author(s)
      Sugimoto K, Yajima H, Hayashi Y, Minato D, Terasaki S, Tohda C, Matsuya Y.
    • Journal Title

      Organic Lett.

      Volume: 17(23) Issue: 23 Pages: 5910-5913

    • DOI

      10.1021/acs.orglett.5b03138

    • Related Report
      2015 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Presentation] アルツハイマー症治療薬開発を指向した Denosomin-Vitamin D3 ハイブリッドの設計と合成2016

    • Author(s)
      村田 賢信, 矢島 久成, 林 祐介, 湊 大志郎, 寺崎 紗有里, 杉本 健士, 東田 千尋, 松谷裕二
    • Organizer
      日本薬学会第136年会
    • Place of Presentation
      横浜
    • Year and Date
      2016-03-27
    • Related Report
      2015 Annual Research Report
  • [Presentation] Design, synthesis, and biological evaluation of promising anti-Alzheimer’s compounds having dihydropyrone unit as a key component.2015

    • Author(s)
      Sugimoto K, Yajima H, Tohda C, Matsuya Y.
    • Organizer
      The XVI International Conference on Heterocycles in Bioorganic Chemistry
    • Place of Presentation
      Metz (France)
    • Year and Date
      2015-06-08
    • Related Report
      2015 Annual Research Report
    • Int'l Joint Research
  • [Presentation] 創薬に生かされている化学2014

    • Author(s)
      松谷裕二
    • Organizer
      高教研大会化学部会
    • Place of Presentation
      富山
    • Year and Date
      2014-10-02
    • Related Report
      2014 Research-status Report
    • Invited
  • [Presentation] 生理活性天然物を基盤とした分子設計と有機合成2014

    • Author(s)
      松谷裕二
    • Organizer
      東邦大学特別セミナー講演会
    • Place of Presentation
      千葉
    • Year and Date
      2014-06-14
    • Related Report
      2014 Research-status Report
    • Invited
  • [Presentation] 新規神経系賦活薬創成を目指したデノソミン-Vitamin D3ハイブリッドの合成2013

    • Author(s)
      矢島久成,杉本健士,東田千尋,湊大志郎,松谷裕二
    • Organizer
      有機合成化学北陸セミナー
    • Place of Presentation
      金沢
    • Related Report
      2013 Research-status Report
  • [Presentation] デノソミン-VD3ハイブリッドの設計と合成を基盤とした新規アルツハイマー治療薬の開発研究2013

    • Author(s)
      矢島久成,杉本健士,湊大志郎,東田千尋,松谷裕二
    • Organizer
      第43回複素環化学討論会
    • Place of Presentation
      岐阜
    • Related Report
      2013 Research-status Report

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Published: 2014-07-25   Modified: 2019-07-29  

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