Aromatic Diboronic Acids as Effective KPC/AmpC Inhibitors.

ABSTRACT: Over 30 compounds, including para-, meta-, and ortho-phenylenediboronic acids, ortho-substituted phenylboronic acids, benzenetriboronic acids, di- and triboronated thiophenes, and pyridine derivatives were investigated as potential β-lactamase inhibitors. The highest activity against KPC-type carbapenemases was found for ortho-phenylenediboronic acid 3a, which at the concentration of 8/4 mg/L reduced carbapenems' MICs up to 16/8-fold, respectively. Checkerboard assays revealed strong synergy between carbapenems and 3a with the fractional inhibitory concentrations indices of 0.1-0.32. The nitrocefin hydrolysis test and the whole cell assay with E. coli DH5α transformant carrying bla_KPC-3 proved KPC enzyme being its mo

SUBMITTER: Krajewska J 

PROVIDER: S-EPMC10648349 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature