Aza-boronic acids as non-beta-lactam inhibitors of AmpC-beta-lactamase
| Autor: | Valentina Buzzoni, Samuele Calò, Alberto Venturelli, Jesús Blázquez, Stefania Ferrari, M. Paola Costi |
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| Rok vydání: | 2003 |
| Předmět: |
Gram-negative bacteria
Stereochemistry Clinical Biochemistry Pharmaceutical Science Ceftazidime medicine.disease_cause antinfectives beta lacatmase azaboronic acids Biochemistry beta-Lactamases Minimum inhibitory concentration chemistry.chemical_compound Bacterial Proteins Drug Discovery medicine Escherichia coli Enzyme Inhibitors Molecular Biology Clavulanic Acid Cephalosporin Antibiotic chemistry.chemical_classification Aza Compounds biology Molecular Structure Organic Chemistry biology.organism_classification Boronic Acids Enzyme chemistry Enzyme inhibitor biology.protein Lactam Molecular Medicine beta-Lactamase Inhibitors medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 14(15) |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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