Development of neuroprotective agents useful for the prevention and improvement of dementia

2023 Fiscal Year Final Research Report

• Project/Area Number: 21K05407
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 38040:Bioorganic chemistry-related
• Research Institution: Osaka Institute of Technology
• Principal Investigator: Kobayashi Shoji 大阪工業大学, 工学部, 准教授 (30374903)
• Co-Investigator(Kenkyū-buntansha): 長井 薫 千里金蘭大学, 生活科学部, 教授 (20340953)
• Project Period (FY): 2021-04-01 – 2024-03-31
• Keywords: 抗認知症 / 神経保護剤 / 天然物 / 合成 / グリーンケミストリー / きのこ / 紅藻 / 構造活性相関

Outline of Final Research Achievements

This study focused on the chemical synthesis of natural products isolated from fungi and algae, and green synthesis of a known antidementia drug to develop neuroprotective agents useful for the prevention and improvement of dementia and to offer new production method of antidementia drug. The collective synthesis of geranyl-resorcinols and sterols isolated from mushrooms were achieved, and some molecules were found to possess neuroprotective activity. We also developed a new method for constructing a bromine-containing bicyclic ether for the purpose of synthesizing natural products derived from red algae. Regarding the green synthesis, an efficient one-pot reaction converting primary alcohols to protected amines was developed, which culminated in the green synthesis of memantine hydrochloride that is currently used worldwide as the anti-dementia drug.

Free Research Field

Synthetic organic chemistry

Academic Significance and Societal Importance of the Research Achievements

本研究は，きのこや海藻の機能に関わる低分子成分の安定供給，構造決定，生物活性の解明に役立ち，天然食材の機能を成分化学的見地で理解・裏付ける根拠として意義がある。また，認知症予防に役立つ可能性のある神経保護剤を天然分子から発掘・創造する上で有用な知見を与える。研究過程で得られた分子構築法や反応手法は，既知の医薬品を含む様々な有機分子の合成に応用でき，有機合成化学の発展に広く貢献する。