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非ペプチドール神経向性変調剤である (+/-) -ジアディフェニンの全合成

Young Shin Cho¹, David A Carcache, Yuan Tian

¹Laboratory for Bioorganic Chemistry and Laboratory of Biochemistry and Pharmacology, Sloan-Kettering Institute for Cancer Research, 1275 York Avenue, New York, New York 10021, USA.

Journal of the American Chemical Society

|November 4, 2004

まとめ

研究者は,ジアディフェニンの最初の完全合成を達成した (1). 合成の中間物質である化合物17は,優れた神経栄養活性を示し,薬剤発見のための有望な道を提供した.

科学分野:

有機化学オーガニック・ケミストリー
神経科学は神経科学である.
薬用化学薬用化学について

背景:

ジアディフェニン (1) は,潜在的な治療用途を持つ天然製品です.
以前の合成経路は限られたか不完全であった.
その生物学的活性を理解することは,薬の開発に極めて重要です.

研究の目的:

ジアディフェニンの最初の完全合成を達成するために (1).
ジアディフェニンとその類似体の生物学的活性を評価する方法を確立する.
強化された神経栄養特性を有する新しい化合物を特定する.

主な方法:

新種の合成戦略を用いたジアディフェニンの総合合成 (1)
ニューロトロフィック活性評価のための生物学的測定法の開発.
化合物17を含む主要な中間物質の合成と評価

主要な成果:

ジアディフェニンの最初の完全合成が成功しました (1).
生物学的評価のための信頼できるプラットフォームの確立.
合成中間物質である化合物17は,ジアディフェニン (1) と比較して,神経栄養活性が著しく増加した.

結論:

現在,ジアディフェニンの全合成 (1) が可能になっています.
合成中介物質は,強力な生物学的活性を持つことができます.
化合物17は,新しい神経栄養薬の開発に有望なリードを代表しています.

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