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Naphthyl Tetronic Acids as Multi-Target Inhibitors of Bacterial Peptidoglycan Biosynthesis

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Abstract

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A pathway screen targeting multiple muramyl peptide synthesis inhibitors identified the naphthyl tetronic acids series. Optimization of this series based on IC50, Kd and MIC values led to potent inhibitors. Compound 5 h was co-crystallized in the active site of E. coli Mur B.

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