Abstract
The synthesis of a selected set of 6-bromopenicillanic acid derivatives with an additional C6 substituent is reported. All these substances were tested as inhibitors of class A and C β-lactamase enzymes derived from Escherichia coli (TEM-1) and E. cloacae (P99). As 6-(1-hydroxyethyl) derivatives 4c and 6c were found to be weak β-lactamase inhibitors, they were further investigated in combination with amoxicillin against a series of β-lactamase-producing bacterial strains. Some structure-activity relationships are discussed.
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