| Autor: |
Uri JV, Actor P, Zajac I, Pitkin DH, Phillips L, Guarini JR, Bartus HF, Polansky TJ, Dunn GL, Hoover JR, Weisbach JA |
| Jazyk: |
angličtina |
| Zdroj: |
The Journal of antibiotics [J Antibiot (Tokyo)] 1979 Nov; Vol. 32 (11), pp. 1161-7. |
| DOI: |
10.7164/antibiotics.32.1161 |
| Abstrakt: |
Three cephalosporins with 7-(2-hydroxyiminophenylacetamido) side chains (SK&F 79433, 80000 and 80303), differing in their 3-substituents, exhibited similar broad-spectrum antibacterial activity in vitro against strains of Staphylococcus aureus, Streptococcus faecalis and various Gram-negative bacilli. All three were active in vivo (s.c., mouse) against S. aureus, Escherichia coli or Klebsiella pneumoniae, but they differed significantly in serum pharmacokinetic profiles. SK&F 80303 produced high and extremely prolonged serum levels and protected mice when administered up to 24 hours prior to challenge with beta-lactamase-producing S. aureus or K. pneumoniae. It was resistant to hydrolysis by beta-lactamases from S. aureus, and variably so to beta-lactamases from E. coli strains. SK&F 80303 was bacteriolytic to logarithmically growing S. aureus, E. coli, Proteus mirabilis, K. pneumoniae and Enterobacter cloacae (partially). SK&F 80303 illustrates further the effect of the 3-sulfoalkyltetrazole substituent on the pharmacokinetic properties of cephalosporins. Its combined biological properties make it a possible candidate for therapeutic and long-term prophylactic use. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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