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新しいマクロリド抗生物質の発見のためのプラットフォーム
Ian B Seiple1, Ziyang Zhang1, Pavol Jakubec1
1Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA.
Nature
|May 20, 2016
まとめ
ソリトロマイシンを含む新しいマクロリド抗生物質候補の作成を可能にする新しい完全合成経路です. このアプローチは細菌の耐性を克服し 新しい抗生物質の発見と製造のプラットフォームを提供します
科学分野:
- 有機化学
- 薬剤化学
- 微生物学
背景:
- 複雑な発酵製品の半合成は 抗生物質の発見に不可欠です
- バクテリアの耐性により,既存のマクロリド抗生物質の有効性が低下しています.
研究 の 目的:
- マクロライド抗生物質の 実践的で完全に合成された経路を開発する
- 伝統的な方法では入手できない多様なマクロリド構造の合成を可能にします.
主な方法:
- 単純な化学的構成要素の収束した組み立て
- 300以上の新しいマクロリド抗生物質候補と臨床候補ソリトロマイシンを合成した.
主要な成果:
- 開発された収束的アプローチは,多様なマクロリド構造の合成を可能にします.
- 合成された化合物のほとんどは抗生物質の活性を示した.
- いくつかの化合物は,現在のマクロリドに耐性のある細菌株に対して有効でした.
結論:
- 記述された化学は,新しいマクロリド抗生物質の発見のための汎用的なプラットフォームを提供します.
- この合成戦略は新しい抗生物質の製造にも適用できるかもしれません
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