シリコン含有窒素ヘテロサイクルの合成,反応性,機能化およびADMET特性

Scott J Barraza¹, Scott E Denmark¹

¹Roger Adams Laboratory, Department of Chemistry , University of Illinois , Urbana , Illinois 61801 , United States.

Journal of the American Chemical Society

|May 16, 2018

まとめ

シリコンは薬剤の設計に独特の利点を提供し,効能と特性を改善します. 新しい方法は,生物学的評価のための様々なシリコンを含む薬剤候補の合成を可能にします.

科学分野:

薬剤化学
薬物の発見
オルガノシリコン化学

背景:

シリコン化合物の合成方法が限られているため,薬剤設計におけるシリコンの潜在力は十分に活用されていない.
独特のシリコン特性により,薬剤の効能と物理化学/ADMETプロファイルが向上します.

研究の目的:

薬剤候補にシリコンを組み込むための新しい合成戦略を開発する.
薬の発見のための様々なシリコンを含む窒素ヘテロサイクルを作成します.
シリコンを含む化合物の生物学的性質を評価する.

主な方法:

シリコン含有テトラヒドロキノリンとテトラヒドロイソキノリンの柔軟な,マルチグラムスケールの合成の開発.
機能化されたシリコンを含む窒素ヘテロサイクルを迅速に構築するための一般的な反応の適応.
選択されたシリコン化合物とその炭素類のADMETに焦点を当てた比較生物学的な研究.

主要な成果:

シリコンを含む新しい構成要素とヘテロサイクルの合成に成功した.
オーガノシリコン製薬の迅速な多様化のための新しい方法の有用性が実証された.
シリコンがADMETの性質に与える影響についての洞察を提供する最初の生物学的データ.

結論:

新しい構成要素戦略により,様々なシリコンを含む薬剤候補の合成が容易になります.
オルガノシリコン化合物は薬剤の性能を改善する見込みがあり,さらなる研究が必要である.
この研究は重要な合成のギャップを解決し薬剤設計におけるシリコンのより広範な利用の道を開きます

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