β-Lactamase-stable penicillins. Synthesis and structure–activity relationships of (Z)-alkyloxyimino penicillins; selection of BRL 44154

Autor:	J. D. Hinks, Richard L. Elliot, Michael J. Pearson, Suzanne C. Cosham, A. John Eglington, John Lowther, John V. Syms, Pauline C. A. Chapman, Roger J. Ponsford, Michael Anthony Harris, David J. Merrikin, Pamela Brown, Stephen H. Calvert
Rok vydání:	1991
Předmět:	chemistry.chemical_classification Unexpected finding Bicyclic molecule Stereochemistry Chemistry Staphylococcus aureus medicine Biological activity Antibacterial activity medicine.disease_cause Alkyl Antibacterial agent
Zdroj:	J. Chem. Soc., Perkin Trans. 1. :881-891
ISSN:	1364-5463 0300-922X
DOI:	10.1039/p19910000881
Popis:	A series of (Z)-2-alkyloxyimino-2-(2-aminothiazol-4-yl)acetamidopenicillins has been prepared. New methodology has been developed to prepare tertiary alkyl oximes. High stability to β-lactamases and potent antibacterial activity have been achieved against Gram-positive and certain Gram-negative organisms. Activity against methicillin-resistant Staphylococcus aureus was an unexpected finding. The cyclopentyl analogue 4f, BRL 44154, has been selected for further study.
Databáze:	OpenAIRE
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