The synthesis and evaluation of 2-substituted-7-(alkylidene)cephalosporin sulfones as beta-lactamase inhibitors

A series of 2-substituted-7-(alkylidene)cephalosporin sulfones were prepared and evaluated as beta-lactamase inhibitors. Compound 11c showed excellent activity as an inhibitor of the class C beta-lactamase derived from Enterobacter cloacae, strain P99.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2000-05, Vol.10 (9), p.847-851
Hauptverfasser:	Buynak, J D, Doppalapudi, V R, Rao, A S, Nidamarthy, S D, Adam, G
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkenes - chemical synthesis Alkenes - pharmacology beta-Lactamase Inhibitors beta-Lactamases Cephalosporins - chemical synthesis Cephalosporins - pharmacology Enterobacter cloacae - drug effects Enterobacter cloacae - enzymology Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Staphylococcus aureus - drug effects Staphylococcus aureus - enzymology Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	A series of 2-substituted-7-(alkylidene)cephalosporin sulfones were prepared and evaluated as beta-lactamase inhibitors. Compound 11c showed excellent activity as an inhibitor of the class C beta-lactamase derived from Enterobacter cloacae, strain P99.
ISSN:	0960-894X
DOI:	10.1016/S0960-894X(00)00094-9