CGP 9000: A new orally active, broad-spectrum cephalosporin.

Zak, O.; Vischer, W. A.; Schenk, C.; Tosch, W.; Zimmermann, W.; Regös, J; Suter, Emanuel; Kradolfer, F; Gelzer, J

doi:10.7164/antibiotics.29.653

Cited by 21 publications

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“…Various oral cephem antibiotics having relatively broad antibacterial spectra have been developed and used worldwide (2, 3, 15,18,19,34). The effectiveness, however, of the oral antibiotics in the treatment of bacterial infections is somewhat limited because of their poor activity against gram-negative bacilli, in particular against opportunistic pathogens belonging to the Enterobacteriaceae or Pseudomonadaceae.…”

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“…R-3746 showed high affinity for penicillinbinding proteins 1, 3, and 4 of Staphylococcus aureus and 1A, 1l$s, and 3 of Escherichia coli. Systemic infections in mice caused by various pathogens, including j3-lactamase-producing strains, responded well to therapy with oral doses of CS-807.Various oral cephem antibiotics having relatively broad antibacterial spectra have been developed and used worldwide (2, 3,15,18,19,34 Fig. 1.…”

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“…Various oral cephem antibiotics having relatively broad antibacterial spectra have been developed and used worldwide (2, 3,15,18,19,34 Fig. 1.…”

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In vitro and in vivo antibacterial activities of CS-807, a new oral cephalosporin

Utsui¹,

Inoue²,

Mitsuhashi³

1987

Antimicrob Agents Chemother

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clinical isolates to R-3746 was determined by the agar dilution method. Ninety percent or more of pathogens such as Staphylococcus aureus, streptococci, Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, indole-positive and indole-negative Proteus spp., Providencia rettgeri, and Haemophilus influenzae were inhibited at concentrations ranging from .0.01 to 1.56 ,ug/ml. Furthermore, at a concentration of 3.13 ,ug/ml, 50% or more of Staphylococcus epidermidis, Morganella morganii, Citrobacterfreundii, and Serratia marcescens strains were also inhibited. Pseudomonas aeruginosa and Xanthomonas maltophilia were resistant to R-3746.The activity of R-3746 was scarcely influenced by several growth conditions. R-3746 was highly resistant to hydrolysis by Il-lactamases derived from various species of bacteria. Killing-curve studies demonstrated bactericidal activity of R-3746 at concentrations above the MIC. R-3746 showed high affinity for penicillinbinding proteins 1, 3, and 4 of Staphylococcus aureus and 1A, 1l$s, and 3 of Escherichia coli. Systemic infections in mice caused by various pathogens, including j3-lactamase-producing strains, responded well to therapy with oral doses of CS-807.Various oral cephem antibiotics having relatively broad antibacterial spectra have been developed and used worldwide (2, 3,15,18,19,34 Fig. 1.The present report deals with the in vitro antibacterial activity of R-3746 together with the therapeutic effect of CS-807 on systemic infections in mice compared with cefaclor, amoxicillin, cefixime, and T-2588 (T-2525).* Corresponding author. MATERIALS AND METHODSChemicals. CS-807 and R-3746 were prepared by Sankyo Co., Ltd., Tokyo, Japan. The other antibiotics were gifts: penicillin G, amoxicillin, and methicillin from Banyu Pharmaceutical Co., Ltd., Tokyo, Japan; cephaloridine from Nihon Glaxo Co., Ltd., Tokyo, Japan; cefaclor from Shionogi & Co., Ltd., Osaka, Japan; cefixime from Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan; and T-2588 and T-2525 from Toyama Chemical Co., Ltd., Tokyo, Japan. All antibiotics were prepared daily with distilled water to the desired concentrations. '4C-labeled penicillin G (potassium 6-phenyl [1-_4C]

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In vitro and in vivo antibacterial activities of CS-807, a new oral cephalosporin

Utsui¹,

Inoue²,

Mitsuhashi³

1987

Antimicrob Agents Chemother

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“…After stirring for 30 minutes, the mixture was diluted with 100ml of water and extracted with ethyl acetate. The extract was concentrated to give 760 mg (37%) of the J-3-cephem as a pale yellow solid; XH NMR (CDC13) 36.93 (1H, s, CHPh2), 6.30 (1H, s, 7=9Hz, NH), 5.82 (1H, dd, 7=9 and 5Hz, C-7), 4.96 (1H, d, 7=5Hz, C-6 OCT. 1991…”

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Synthesis and biological activity of novel 3-(2-propenyl)-cephalosporins. I.

Kim

et al. 1991

J. Antibiot.

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The synthesis, antibacterial activity and oral absorption of novel cephalosporins (3a~3d) having a 2-propenyl group at the C-3 position are described. Diphenylmethyl 7-amino-3-(2-propenyl)-3-cephem-4-carboxylate HC1(4) prepared from 7-aminocephalosporanic acid in 12 steps was acylated with various acid moieties to give cephems 3a~3d. The cephems 3a~3c showedsimilar antibacterial activities as cefixime. However,these cephemswere not well absorbed orally.

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“…Cephalexin (4), cefadroxil (7), cefaclor (4,21), cefroxadine (34), and cefatrizine (22) have been widely used for clinical purposes as oral cephalosporins, but their usage is limited because they have relatively narrow spectra against various strains of pathogenic bacteria and are hydrolyzed by 1-lactamases. BK-218, 5-thia-1-azabicyclo [ Fig.…”

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In vitro investigation of BK-218, a new oral and parenteral cephalosporin

Szabó

Barabás

Tar

et al. 1990

Antimicrob Agents Chemother

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The antibacterial activity of BK-218 was similar to that of cefamandole when it was tested against several laboratory strains. The inhibiting effect of BK-218 was greater than that of cephalexin and cefoxitin on penicillin-binding proteins of Escherichia col HB101. This result was in close correlation with the relative inhibition of radiolabeled glucosamine incorporation (greatest with BK-218) and with the lytic effect (most intensive with BK-218). BK-218 proved to be a good inhibitor for all five of the ,-lactamases that were investigated, although two enzymes (Enterobacter cloacae P99 and Pseudomonas aeruginosa Cilote) hydrolyzed it to some extent.Cephalexin (4), cefadroxil (7), cefaclor (4,21), cefroxadine (34), and cefatrizine (22) (Fig. 1.), is a new oral cephalosporin.It is well-known that beta-lactam antibiotics first bind to their targets, the so-called penicillin-binding proteins (PBPs). The inhibition of these enzymes suspends peptidoglycan synthesis, and as a consequence the autolytic enzymes are triggered with a mechanism whose details are not completely understood (16).The purpose of this study was to report the results of preliminary investigations concerning the in vitro activity of BK-218 against a limited number of gram-positive and gramnegative bacteria. The MICs of BK-218 were compared with those of other parenteral (cefuroxime, cefamandole, and cefoxitin) and oral (cephalexin) antibiotics.The in vitro effect on the targets was measured by (i) affinity to PBPs, (ii) incorporation of labeled glucosamine into the cell wall of Escherichia coli, and (iii) release of labeled glucosamine-containing fragments from prelabeled cell wall of E. coli to assess the lysis capability of BK-218.

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CGP 9000: A new orally active, broad-spectrum cephalosporin.

Cited by 21 publications

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In vitro and in vivo antibacterial activities of CS-807, a new oral cephalosporin

In vitro and in vivo antibacterial activities of CS-807, a new oral cephalosporin

Synthesis and biological activity of novel 3-(2-propenyl)-cephalosporins. I.

In vitro investigation of BK-218, a new oral and parenteral cephalosporin

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