Substituted 6-alkyloxapenems: potent β-lactamase inhibitors: synthesis and biological characterization

The synthesis of 6-alkyloxapenems bearing hydroxy, fluorine, amino, acylamino and sulfonamido substituents in the 1'-position is described. Several of the compounds are potent inhibitors of β-lactamases from Staphylococcus aureus and Proteus vulgaris and have an appreciable stability against ch...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1993-11, Vol.3 (11), p.2205-2210
Main Authors: Wild, Hanno, Metzger, Karl-Georg
Format: Article
Language:English
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Summary:The synthesis of 6-alkyloxapenems bearing hydroxy, fluorine, amino, acylamino and sulfonamido substituents in the 1'-position is described. Several of the compounds are potent inhibitors of β-lactamases from Staphylococcus aureus and Proteus vulgaris and have an appreciable stability against chemical hydrolysis. The synthesis of oxapenems bearing various substituted alkyl residues in the 6-position is described. Several of the compounds are potent inhibitors of β-lactamases from Staphylococcus aureus and Proteus vulgaris and have an appreciable stability against chemical hydrolysis.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)80926-4