Abstract
Experiments were conducted that showed Staphylococcusaureusβ-lactamase activity to be inhibited the most by dicloxacillin, cephaloglycin, and 7-ACA, to a lesser degree by cloxacillin, quinacillin, oxacillin, 6-APA, cephalexin, nafcillin, and ancillin and least of all by methicillin. Bacillus cereus β-lactamase activity was inhibited most by nafcillin and dicloxicillin and only moderately by all the other inhibitors cited, including methicillin, which was least effective. The degree of inhibition was shown to depend on the structural characteristics of the inhibitor, the time of exposure of enzyme to inhibitor, and the ratio of amount of inhibitor to amount of substrate. The inhibition was of the competitive type. The compounds having the highest affinity for the enzyme or the lowest Ki value were the strongest inhibitors and were most effective in protecting the susceptible substrate from hydrolysis.
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