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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- 1.Neu HC: Beta-lactam antibiotics: structural relationships affecting in vitro activity and pharmacologic properties. Reviews of Infectious Diseases 1986, 8, Supplement 3: 237–259.Google Scholar
- 2.White DR, Davenport LC: Antibacterial agents. In: Bristol JA (ed): Annual reports in medicinal chemistry, volume 25. Academic Press, London, 1990, p. 109–118.Google Scholar
- 3.Brighty KE, McGuirk PR: Antibacterial agents. In: Bristol JA (ed): Annual reports in medicinal chemistry, volume 25. Academic Press, London, 1990, p. 123–132.Google Scholar
- 4.National Committee for Clinical Laboratory Standards: Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically. Approved Standard M7A2. NCCLS, Villanova, PA, 1990.Google Scholar
- 5.Pearson PD, Steigbigel RT, Davis HT, Chapman SW: Method for reliable determination of minimal lethal concentrations. Antimicrobial Agents and Chemotherapy 1980, 18: 699–708.Google Scholar
- 6.Neu HC: Antibiotic inactivating enzymes and bacterial resistance. In: Lorian V (ed): Antibiotics in laboratory medicine. Williams & Wilkins, Baltimore, 1986, p. 757–789.Google Scholar
- 7.Jones RN, Erwin ME, Barrett MS, Briggs BM, Johnson DM: In vitro activity of RU29246, the metabolite of a new HR916 cephalosporin ester. Diagnostic Microbiology and Infectious Disease 1991, 14: 473–483.Google Scholar
- 8.Jones RN, Washington, JA, Pfaller MA, Koontz FP, Gerlach EH, Erwin MF: Quality control guidelines for haemophilus test medium MIC susceptibility tests with cefmetazole, cefpodoxime, CI-960 (PD127391, AM-1090), and RU29246. Journal of Antimicrobial Chemotherapy 1991, 27: 390–392.Google Scholar
- 9.Murray PR, Allen SD, Erwin ME, Gerlach EH, Jones RN, Koontz FP, Pfaller MA, Washington JA: Antimicrobial activity of RU 29246 (HR 916 metabolite) compared with four other oral beta-lactams tested against more than 5000 clinical isolates. European Journal of Clinical Microbiology and Infectious Diseases 1991, 10: 776–781.Google Scholar