The Journal of Antibiotics
Online ISSN : 1881-1469
Print ISSN : 0021-8820
ISSN-L : 0021-8820
BIOLOGICAL AND CHEMOTHERAPEUTIC STUDIES ON THREE SEMISYNTHETIC CEPHAMYCINS
JOSEPH V. URIPAUL ACTORJOSEPH R. GUARINILILLIAN PHILLIPSDONALD PITKINROBERT M. DEMARINISJERRY A. WEISBACH
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1978 Volume 31 Issue 1 Pages 82-91

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Abstract

Three semisynthetic cephamycin antibiotics (7α-methoxy-cephalosporins), SKF 73678, SK&F 83088 (CS-1170) and cefoxitin, have been found to possess favorable biological and chemotherapeutic properties. All three cephamycins are active In vitro against strains of Staphylococcus aureus and a variety of gram-negative bacilli. Beta-lactamase producing organisms including indole-producing Proteus spp., Enterobacter spp. and Serratia strains as well as certain anaerobic bacteria were found to be susceptible to these antibiotics. SK & F 73678 showed somewhat better MIC values than cefoxitin against multiple strains of bacteria. Strains of Pseudonionas aeruginosa and group D streptococci are essentially insensitive to these compounds. Their binding to serum proteins is relatively low. In mice, cefoxitin showed the most favorable pharmacokinetics with respect to peak serum level, serum half-life and urinary recovery. These cephamycins protected mice experimentally infected with a variety of bacterial strains. All three compounds are rapidly bacteriolytic to the logarithmically growing Escherichia coli and belatedly so to Staphylococcus strains with complete sterilizing effect. SK&F 73678 and SK&F 83088 showed activity and potency comparable to or better than cefoxitin and thus can be considered candidates for clinical study.

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© Japan Antibiotics Research Association
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