Cefatrizine Activity Compared with That of Other Cephalosporins

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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confidence: 99%

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confidence: 99%

See 1 more Smart Citation

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

Utsui¹,

Inoue²,

Mitsuhashi³

1987

“…Oral cephalosporins such as cephalexin (1), cefaclor (1,16), cefatrizine (17), cefadroxil (3), and cefroxadine (28) have been developed and used widely for clinical purposes. However, they have a relatively narrow spectrum against pathogens and are hydrolyzed by various types of Plactamases.…”

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confidence: 99%

In vitro and in vivo antibacterial activities of T-2588, a new oral cephalosporin, compared with those of other oral beta-lactam antibiotics

Okamoto¹,

Hamana²,

Inoue³

et al. 1987

T-2588, the pivaloyloxymethyl ester of T-2525, [6R, 7R]-7-[(z)-2-(2-aminothiazol-4-yl)-2-methoxyiminoacetoamido] -3- [(5-methyl-2H-tetrazol-2-yl)methyl]-3-cephem-4-carboxylic acid, is a new oral cephalosporin. T-2525 had a widely expanded antibacterial spectrum against gram-negative and gram-positive bacteria. T-2525 was more active in vitro than cefaclor, cephalexin, and amoxicillin against members of the family Enterobacteriaceae and Branhamella catarrhalis. Moreover, it exhibited superior in vitro activity against Streptococcus pyogenes, Streptococcus pneumoniae, Haemophilus influenzae, and Neisseria gonorrhoeae. T-2525 was highly stable to various beta-lactamases, which were classified as Richmond and Sykes types Ia, Ib, Ic, III, IV, and Vc. It had high affinities for the lethal (essential) penicillin-binding proteins of Escherichia coli, Clostridium perfringens, and Bacteroides fragilis. T-2588 had excellent therapeutic effect on systemic infections in mice with various species of gram-negative bacteria, including beta-lactamase-producing bacteria.

“…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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confidence: 99%

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

Szabó

Barabás

Tar

et al. 1990

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.