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Farmaco. 2002 Aug;57(8):663-9.

Synthesis and biological evaluation of 6-bromo-6-substituted penicillanic acid derivatives as beta-lactamase inhibitors.

Author information

1
Istituto di Chimica Farmaceutica, Università di Urbino, Italy. annalida@uniurb.it

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 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.

PMID:
12361234
DOI:
10.1016/s0014-827x(02)01261-2
[Indexed for MEDLINE]

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