Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus

Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus

The synthesis and antimicrobial activity of several new 1-carba-1-dethiacephalosporins is described. The discovery of unique activity of some of the analogues against methicillin-resistant Staphylococcus aureus led to the development of a structure-activity relationship designed to optimize this act...

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Veröffentlicht in:Journal of medicinal chemistry 1993-07, Vol.36 (14), p.1971-1976
Hauptverfasser: Ternansky, Robert J, Draheim, Susan E, Pike, Andrew J, Bell, F. William, West, Sarah J, Jordan, Christopher L, Wu, C. Y. Ernie, Preston, David A, Alborn, William
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacokinetics
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Biological and medical sciences
Blood Proteins - metabolism
Cephalosporins - chemical synthesis
Cephalosporins - pharmacokinetics
Cephalosporins - pharmacology
Half-Life
Humans
Macaca mulatta
Male
Medical sciences
Methicillin Resistance
Mice
Mice, Inbred ICR
Microbial Sensitivity Tests
Pharmacology. Drug treatments
Rats
Rats, Sprague-Dawley
Staphylococcus aureus - drug effects
Structure-Activity Relationship
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Beschreibung
Zusammenfassung:The synthesis and antimicrobial activity of several new 1-carba-1-dethiacephalosporins is described. The discovery of unique activity of some of the analogues against methicillin-resistant Staphylococcus aureus led to the development of a structure-activity relationship designed to optimize this activity. The results of this investigation along with the pharmacokinetic characteristics of select compounds are described.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00066a006