Inhibition of light-induced stomatal opening with aromatic amines

2021 Fiscal Year Final Research Report

• Project/Area Number: 19K22251
• Research Category: Grant-in-Aid for Challenging Research (Exploratory)
• Allocation Type: Multi-year Fund
• Review Section: Medium-sized Section 37:Biomolecular chemistry and related fields
• Research Institution: Kwansei Gakuin University (2020-2021); Nagoya University (2019)
• Principal Investigator: Murakami Kei 関西学院大学, 理学部, 准教授 (90732058)
• Project Period (FY): 2019-06-28 – 2022-03-31
• Keywords: aromatic amination / stomata

Outline of Final Research Achievements

We have developed various C-H amination reactions and, with these reactions in hand, prepared a C-H amination-based arylamine collection. Through phenotype-based screening, we have evaluated the bioactivity of the arylamines towards plant stomata. From the collection, we accomplished the successful identification of the lead candidate SIM1 (a sulfonimidated 2,4-diphenyloxazole) that inhibits light-induced stomatal opening. Further structure-activity relationship (SAR) study allowed us to prepare an array of SIM1 derivatives. This led to the identification of SIM3* (a sulfonamidated oxazole) which showed stronger activity and greater selectivity towards the stomatal opening cascade. Since stomata play an important role in regulating leaf transpiration, it is expected that our research will lead to the development of drought tolerance-conferring agrochemicals.

Free Research Field

有機化学

Academic Significance and Societal Importance of the Research Achievements

本研究は、基礎科学的な有機反応開発によって得られた生成物から、気孔開口を阻害する分子を発見した内容である。特に有機反応開発で行う適用範囲の検討により得られた生成物がそのまま構造活性相関研究に応用可能であり、分子の活性に対する情報を一挙に得られる。反応開発の利点を活かした分野横断的研究であり、有機化学と植物学の共同研究により、新しい生物活性分子を創出した。同様のアプローチは展開が可能であり、今後の発展が期待される。