Synthesis and biological evaluation of 6-bromo-6-substituted penicillanic acid derivatives as β-lactamase inhibitors
2002; Elsevier BV; Volume: 57; Issue: 8 Linguagem: Inglês
10.1016/s0014-827x(02)01261-2
ISSN1879-0569
AutoresAnnalida Bedini, Cesarino Balsamini, Barbara Di Giacomo, Andrea Tontini, Barbara Citterio, Luca Giorgi, Enza Di Modugno, Giorgio Tarzia,
Tópico(s)Pharmaceutical and Antibiotic Environmental Impacts
ResumoThe 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 beta-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 beta-lactamase inhibitors, they were further investigated in combination with amoxicillin against a series of beta-lactamase-producing bacterial strains. Some structure-activity relationships are discussed.
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