Journal
NATURE CHEMISTRY
Volume 4, Issue 10, Pages 789-793Publisher
NATURE PUBLISHING GROUP
DOI: 10.1038/NCHEM.1402
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Funding
- European Union
- Netherlands Organization for Scientific Research (NWO-Vici)
- Netherlands Organization for Scientific Research (NWO-Echo)
- Zernike Institute for Advanced Materials
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Emerging trends in drug discovery are prompting a renewed interest in natural products as a source of chemical diversity and lead structures. However, owing to the structural complexity of many natural compounds, the synthesis of derivatives is not easily realized. Here, we demonstrate a conceptually new approach using oligonucleotides as aptameric protective groups. These block several functionalities by non-covalent interactions in a complex molecule and enable the highly chemo-and regioselective derivatization (>99%) of natural antibiotics in a single synthetic step with excellent conversions of up to 83%. This technique reveals an important structure-activity relationship in neamine-based antibiotics and should help both to accelerate the discovery of new biologically active structures and to avoid potentially costly and cumbersome synthetic routes.
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