A semi-synthetic penicillinase inactivator

MANY pathogenic bacteria secrete penicillinases ( β -lactamases, EC 3.5.2.6) as a defence mechanism against β -lactam antibiotics 1 . Inhibitors of penicillinase are therefore of potential clinical importance, and interest in this area has been stimulated by the discovery of effective naturally occu...

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Bibliographic Details
Published in:Nature (London) 1979-03, Vol.278 (5702), p.360-361
Main Authors: CARTWRIGHT, S. J, COULSON, A. F. W
Format: Article
Language:English
Subjects:
beta-Lactamase Inhibitors
beta-Lactams - pharmacology
Binding Sites
Dose-Response Relationship, Drug
Humanities and Social Sciences
letter
multidisciplinary
Penicillanic Acid - pharmacology
Science
Science (multidisciplinary)
Staphylococcus aureus - enzymology
Structure-Activity Relationship
Sulfones
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Summary:MANY pathogenic bacteria secrete penicillinases ( β -lactamases, EC 3.5.2.6) as a defence mechanism against β -lactam antibiotics 1 . Inhibitors of penicillinase are therefore of potential clinical importance, and interest in this area has been stimulated by the discovery of effective naturally occurring enzyme inactivators 2–4 . We have studied the interaction of one of these, clavulanic acid (I) with the exocellular enzyme from Staphylococcus aureus , and we report here the synthesis of a novel penicillinase inhibitor whose design was based on the mechanism postulated for the inactivation by clavulanate.
ISSN:0028-0836
1476-4687
DOI:10.1038/278360a0