Comparative in vitro activity and beta-lactamase stability of RU29246, the active metabolite of HR916B.
HR 916B is a new orally absorbed cephalosporin. In tests its active metabolite, RU29246, inhibited Streptococcus pyogenes, Streptococcus agalactiae and Streptococcus pneumoniae at less than or equal to 0.12 micrograms/ml, which is similar to the antibacterial activity of cefuroxime, and was more active than cefaclor. It was also more active (MIC 2 micrograms/ml) than cefixime, cefuroxime, cefaclor and cefotaxime against staphylococci. RU29246 inhibited Escherichia coli, Klebsiella pneumoniae, Citrobacter diversus, Klebsiella oxytoca, Proteus mirabilis, Providencia stuartii and Salmonella spp. at less than or equal to 1 microgram/ml, thus being more active than cefuroxime and cefaclor, but was less active than cefixime and cefotaxime. It did not inhibit Pseudomonas aeruginosa and other Pseudomonas spp., Enterobacter spp., Serratia marcescens or Bacteroides fragilis. RU29246 was not hydrolyzed by TEM-1, Staphylococcus aureus TEM-2 or Moraxella catarrhalis beta-lactamases, but was hydrolyzed by TEM-3 and the chromosomal beta-lactamases of Proteus vulgaris and Morganella morganii. Plasmid and chromosomal beta-lactamases were inhibited by RU29246.
Yu
K W
KW
Department of Medicine, College of Physicians & Surgeons, Columbia University, New York, New York 10032.
Chin
N X
NX
Neu
H C
HC
D002511:Cephalosporins / Q000378:metabolism / Q000494:pharmacology*; D004355:Drug Stability; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006868:Hydrolysis; D008826:Microbial Sensitivity Tests; D001618:beta-Lactamases / Q000494:pharmacology*
D002511:Cephalosporins; C073743:RU 29246; D001618:beta-Lactamases