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

Dynamic combinatorial chemistry (DCC) is a powerful tool to identify ligands for biological targets. We used 19 F 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-aroma...

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Published in:Organic & biomolecular chemistry 2018-11, Vol.16 (43), p.8144-8149
Main Authors: Ekström, Alexander G, Wang, Jue Theresa, Bella, Juraj, Campopiano, Dominic J
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Summary:Dynamic combinatorial chemistry (DCC) is a powerful tool to identify ligands for biological targets. We used 19 F 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 ec FabH, 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. Dynamic combinatorial chemistry (DCC) is a powerful tool to identify ligands for biological targets.
ISSN:1477-0520
1477-0539
DOI:10.1039/c8ob01918e