Comparative in vitro activity and beta-lactamase stability of RU29246, the active metabolite of HR916B
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HR 916B is a new orally absorbed cephalosporin. In tests its active metabolite, RU29246, inhibitedStreptococcus pyogenes, Streptococcus agalactiae andStreptococcus pneumoniae at ≤ 0.12 µg/ml, which is similar to the antibacterial activity of cefuroxime, and was more active than cefaclor. It was also more active (MIC 2 µg/ml) than cefixime, cefuroxime, cefaclor and cefotaxime against staphylococci. RU29246 inhibitedEscherichia coli, Klebsiella pneumoniae, Citrobacter diversus, Klebsiella oxytoca, Proteus mirabilis, Providencia stuartii andSalmonella spp. at ≤ 1 µg/ml, thus being more active than cefuroxime and cefaclor, but was less active than cefixime and cefotaxime. It did not inhibitPseudomonas aeruginosa and otherPseudomonas spp.,Enterobacter spp.,Serratia marcescens orBacteroides fragilis. RU29246 was not hydrolyzed by TEM-1,Staphylococcus aureus TEM-2 orMoraxella catarrhalis beta-lactamases, but was hydrolyzed by TEM-3 and the chromosomal beta-lactamases ofProteus vulgaris andMorganella morganii. Plasmid and chromosomal beta-lactamases were inhibited by RU29246.
KeywordsInternal Medicine Antibacterial Activity Staphylococcus Aureus Cephalosporin Active Metabolite
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