ランカシディン抗生物質に対するモジュラーアプローチ
Lingchao Cai1,2, Yanmin Yao2, Seul Ki Yeon2
1Jiangsu Provincial Key Lab for the Chemistry and Utilization of Agro-Forest Biomass, Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, Jinagsu Key Lab of Biomass-Based Green Fuels and Chemicals, Nanjing Forestry University, Nanjing, 210037 Jiangsu, China.
Journal of the American Chemical Society
|August 14, 2020
まとめ
合成化学は新しいランカシジン抗生物質へのアクセスを促進します この研究は既知の化合物の構造を修正し,潜在的な抗菌作用を持つ新しい誘導体を作成します.
科学分野:
- 自然製品 化学
- 合成有機化学
- 薬剤化学
背景:
- ランカシジンは,Streptomyces spp.のポリケチドの天然産物である. * 抗菌能力がある
- 複雑で不安定な構造は 合成と改変に課題を伴う.
- いくつかのランカシジンの以前の構造的割り当ては不正確でした.
研究 の 目的:
- ランカシジンの新合成経路の開発
- 構造的に多様なランカシジンの誘導体を生成し,安定性と活性性を高めます.
- 特定のランカシジンの構造を修正し確認する.
主な方法:
- ランカシジンの3つの異なる全合成戦略の開発
- 循環性および非循環性ランカシジンのステレオ化学的変異の系統的生成.
- 化学的安定性を高めるためにC4メチル化されたランカシジンの合成
主要な成果:
- C4メチル化誘導体を含む様々なランカシジンの合成に成功した.
- 2,18-セコランカシディノールBとイソランカシディノールについて以前に報告された構造の修正
- 新型ランカシジンの抗菌およびタンパク質変換阻害作用の評価
結論:
- 開発された合成経路は,新しいランカシディンの構造的変異へのアクセスを提供します.
- この研究は,重要なランカシジン天然製品の構造的アイデンティティを明確にします.
- 生成された微生物は 改良された抗菌剤を開発するためのプラットフォームを提供します
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