1393446-95-1Relevant academic research and scientific papers
Selective transformations of complex molecules are enabled by aptameric protective groups
Bastian, Andreas A.,Marcozzi, Alessio,Herrmann, Andreas
, p. 789 - 793,5 (2012)
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.
Methods for chemical synthesis of biologically active compounds using supramolecular protective groups and novel compounds obtainable Thereby
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Paragraph 0115; 0116, (2014/09/03)
The invention relates to drug development and synthetic chemistry, in particular to the manufacture of biologically active compounds based on naturally occurring molecules. It also relates to novel biologically active compounds, for example aminoglycoside
