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NMR-Guided Fragment-Based Approach for the Design of AAC(6′)-Ib Ligands

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Abstract

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Reverse n.O.e. pumping in the detection and optimisation of ligands: Ligand-observed NMR experiments have been used to drive the detection and optimisation of non-aminoglycosidic ligands for AAC(6′)Ib, one of the most clinically important resistance enzymes to aminoglycosides. This fragment-based approach has been conducted without any need for NMR structural assignment of the target, and has been validated by the preparation of a bisubstrate inhibitor.

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