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Creation of New Lead Compounds using Natural Resources and Metal Nanoparticle Catalysts

Research Project

Project/Area Number 22K15252
Research Category

Grant-in-Aid for Early-Career Scientists

Allocation TypeMulti-year Fund
Review Section Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
Research InstitutionOsaka University

Principal Investigator

Sirimangkalakitti Natchanun  大阪大学, 大学院薬学研究科, 特任助教 (10909120)

Project Period (FY) 2022-04-01 – 2024-03-31
Project Status Completed (Fiscal Year 2023)
Budget Amount *help
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2023: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Fiscal Year 2022: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000)
Keywordsnatural product extract / chemical diversification / metal catalyst / lead compound
Outline of Research at the Start

Natural products (NPs) play invaluable roles for drug discovery and development. However, during last two decades, the de-emphasis of NP research correlated to overall reduction in new leads and drug approval. To create brand new biologically active compounds from NPs, we set up our methodology by using of diversity-oriented synthesis of NP extracts, via metal nanoparticle catalysts. This synthesis could directly access a number of NP-like compounds in one-step. Our new approach is promising for faster and more efficient drug discovery and development.

Outline of Final Research Achievements

We have developed a methodology for creating and discovering new biologically active compounds using natural resources and highly reactive metal nanoparticle catalysts. Our approach uniquely employs nanoparticle catalysts, such as Pd, to efficiently catalyze C-H bond activation, C-C cleavage, and cross-coupling reactions, facilitating the formation of new natural product-like compounds in one step. Our research successfully demonstrated the direct chemical diversification of natural product extracts from marine sponges, leading to the discovery of a new compound, rac-6-OEt-cylindradine A. These findings underscore the potential of our method for faster and more efficient drug discovery and development. We are further enhancing this methodology by developing highly reactive Rh nanoparticle catalysts. Research Achievements: two peer-reviewed publications and two conference presentations, one at an international conference

Academic Significance and Societal Importance of the Research Achievements

Our research advances drug discovery by using metal nanoparticle catalysts to create new biologically active compounds from natural product extracts. This innovative approach accelerates pharmaceutical development, offering potential treatments for various diseases.

Report

(3 results)
  • 2023 Annual Research Report   Final Research Report ( PDF )
  • 2022 Research-status Report
  • Research Products

    (4 results)

All 2023 2022

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

  • [Journal Article] A New Tetracyclic Bromopyrrole-Imidazole Derivative through Direct Chemical Diversification of Substances Present in Natural Product Extract from Marine Sponge Petrosia (Strongylophora) sp.2022

    • Author(s)
      Sirimangkalakitti Natchanun、Harada Kazuo、Yamada Makito、Arai Masayoshi、Arisawa Mitsuhiro
    • Journal Title

      Molecules

      Volume: 28 Issue: 1 Pages: 143-143

    • DOI

      10.3390/molecules28010143

    • Related Report
      2022 Research-status Report
    • Peer Reviewed / Open Access
  • [Journal Article] Design, Synthesis, and Monoamine Oxidase B Selective Inhibitory Activity of <i>N</i>-Arylated Heliamine Analogues2022

    • Author(s)
      Yamada Makito、Hirose Yu、Lin Bangzhong、Fumimoto Megumi、Nunomura Kazuto、Natchanun Sirimangkalakitti、Takahashi Naoyuki、Ohki Yuuta、Sako Makoto、Murai Kenichi、Harada Kazuo、Arai Masayoshi、Suzuki Sayo、Nakamura Tomonori、Haruta Junichi、Arisawa Mitsuhiro
    • Journal Title

      ACS Medicinal Chemistry Letters

      Volume: 13 Issue: 10 Pages: 1582-1590

    • DOI

      10.1021/acsmedchemlett.2c00228

    • Related Report
      2022 Research-status Report
    • Peer Reviewed
  • [Presentation] A New Tetracyclic Bromopyrrole-Imidazole Derivative through Direct Chemical Diversification of Substances Present in Natural Product Extract from Marine Sponge Petrosia (Strongylophora) sp.2023

    • Author(s)
      Natchanun Sirimangkalakitti
    • Organizer
      The American Society of Pharmacognosy 2023 Annual Meeting Innovation Through Interaction
    • Related Report
      2023 Annual Research Report
    • Int'l Joint Research
  • [Presentation] A New Tetracyclic Bromopyrrole-Imidazole Derivative through Direct Chemical Diversification of Substances Present in Natural Product Extract from Marine Sponge Petrosia (Strongylophora) sp.2023

    • Author(s)
      Natchanun Sirimangkalakitti
    • Organizer
      24th Symposium on the Development and Application of Naturally Occurring Drug Materials
    • Related Report
      2023 Annual Research Report

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Published: 2022-04-19   Modified: 2025-01-30  

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