Clavulanic acid, a novel inhibitor of beta-lactamases.

Antimicrobial agents and chemotherapy ·Vol. 14 ·No. 5 ·1978-11-00 ·Pages 650-5

Neu HC, Fu KP

Abstract

Clavulanic acid, Z-(2R,5R)-3-(beta-hydroxyethylidene)-7-oxo-4-oxa-1-azabicyclo-[3,2,0] heptane-2-carboxylic acid, has been shown to be an effective inhibitor of the beta-lactamases of the Richmond types II, III, IV, and V. Inhibition is a time-dependent reaction and is irreversible. Clavulanic acid had poor antibacterial activity against Staphylococcus aureus, Enterobacteriaceae, and Pseudomonas aeruginosa, with minimal inhibitory levels greater than 25 mug/ml. It did inhibit the majority of Neisseria gonorrhoeae at 0.1 mug/ml and Haemophilus influenzae at 6.3 mug/ml. Clavulanic acid acted synergistically with penicillins and cephalosporins to inhibit beta-lactamase-producing S. aureus and Enterobacteriaceae. Clavulanic acid combined with ampicillin inhibited beta-lactamase-producing N. gonorrhoeae, H. influenzae, Escherichia coli, Salmonella typhi, and Shigella sonnei.

MeSH Terms

Ampicillin/pharmacology Anti-Bacterial Agents/pharmacology Bacteria/drug effects Cephalosporins/pharmacology Drug Synergism Kinetics Microbial Sensitivity Tests beta-Lactamase Inhibitors beta-Lactams/pharmacology

Chemicals

Anti-Bacterial Agents Cephalosporins beta-Lactamase Inhibitors beta-Lactams Ampicillin

Authors & Affiliations

2 authors, click to expand affiliations / ORCID

Neu H C

Fu K P

References (14)

14 references, click to expand

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Article Info

Journal

Antimicrobial agents and chemotherapy

Abbr.

Antimicrob Agents Chemother

ISSN

0066-4804

DOI

10.1128/AAC.14.5.650

Published

1978-11-00

Pages

650-5

Language

English

Region

United States

NLM ID

0315061

PMCID

PMC352529

Subset

External Links

PubMed source DOI: 10.1128/AAC.14.5.650 PMC Full Text View journal details

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Clavulanic acid, a novel inhibitor of beta-lactamases.

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