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  • Title: Aza-boronic acids as non-beta-lactam inhibitors of AmpC-beta-lactamase.
    Author: Buzzoni V, Blazquez J, Ferrari S, Calò S, Venturelli A, Costi MP.
    Journal: Bioorg Med Chem Lett; 2004 Aug 02; 14(15):3979-83. PubMed ID: 15225711.
    Abstract:
    With the aim of improving the ability of non-beta-lactam inhibitors to inhibit AmpC-beta-lactamase, a series of 3-aza-phenyl-boronic acid derivatives was obtained using in parallel synthesis. The molecules were tested against Escherichia coli AmpC-beta-lactamase. The best inhibitors, 3-(2-hydroxy-naphthalen-1-ylazo)-phenyl-boronic acid (12) and 3-(2,4-dihydroxy-naphthalen-1-ylazo)-phenyl-boronic acid (14), showed apparent inhibition constant values (K(i)) of 0.3 and 0.45 microM and increased the potency of the semi-synthetic cephalosporin antibiotic, ceftazidime, lowering its minimum inhibitory concentration (MIC) value of 50%, against Gram-negative bacteria strains, producing high levels of AmpC-beta-lactamase.
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