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Non-invasive 19F NMR analysis of a protein-templated N-acylhydrazone dynamic combinatorial library

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Abstract

Dynamic combinatorial chemistry (DCC) is a powerful tool to identify ligands for biological targets. We used 19F NMR as an in situ, non-invasive technique for measuring the composition of a dynamic combinatorial library (DCL) of N-acylhydrazones (NAHs). An NAH DCL, constructed from a fluoro-aromatic aldehyde and a small set of hydrazides, was targetted at ecFabH, an essential enzyme in bacterial fatty acid biosynthesis. Our NMR analysis identified a tert-butyl NAH as the best binder which was confirmed by enzymatic assay.

Graphical abstract: Non-invasive 19F NMR analysis of a protein-templated N-acylhydrazone dynamic combinatorial library

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Publication details

The article was received on 06 Aug 2018, accepted on 03 Oct 2018 and first published on 04 Oct 2018


Article type: Paper
DOI: 10.1039/C8OB01918E
Citation: Org. Biomol. Chem., 2018, Advance Article
  • Open access: Creative Commons BY license
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    Non-invasive 19F NMR analysis of a protein-templated N-acylhydrazone dynamic combinatorial library

    A. G. Ekström, J. T. Wang, J. Bella and D. J. Campopiano, Org. Biomol. Chem., 2018, Advance Article , DOI: 10.1039/C8OB01918E

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