In vitro evaluation of E1040, a new cephalosporin with potent antipseudomonal activity. 1988

N Watanabe, and K Katsu, and M Moriyama, and K Kitoh
Department of Microbiology, Tsukuba Research Laboratories, Eisai Co. Ltd., Ibaraki, Japan.

E1040 is a new parenteral cephalosporin with a broad antibacterial spectrum and potent antipseudomonal activity. The compound was four- to eightfold more active than ceftazidime and cefsulodin against Pseudomonas aeruginosa (MIC of E1040 for 90% of strains tested [MIC90], 3.13 micrograms/ml). E1040 also showed a potent activity against other glucose-nonfermentative rods, including Acinetobacter species. The activities of E1040 against most species of the family Enterobacteriaceae were roughly comparable to the activities of ceftazidime and cefmenoxime and exceeded that of cefotiam. Against Citrobacter freundii (MIC90, 0.78 micrograms/ml), Enterobacter cloacae (MIC90, 3.13 micrograms/ml), and Enterobacter aerogenes (MIC90, 0.2 micrograms/ml), E1040 was 16- to 256-fold more active than ceftazidime and cefmenoxime. The activities of E1040 against gram-positive cocci and anaerobes were comparable to those of ceftazidime, but the compound was less active than cefmenoxime. E1040 was at least as resistant as ceftazidime and cefmenoxime to hydrolysis by various beta-lactamases and showed high affinities for penicillin-binding protein 3 of both Escherichia coli and P. aeruginosa.

UI MeSH Term Description Entries
D008712 Methicillin One of the PENICILLINS which is resistant to PENICILLINASE but susceptible to a penicillin-binding protein. It is inactivated by gastric acid so administered by injection. Penicillin, Dimethoxyphenyl,Methicillin Hydrate, Monosodium Salt,Methicillin Monohydrate, Monosodium Salt,Methicillin Sodium,Meticillin,Metin,Staphcillin,Dimethoxyphenyl Penicillin
D010458 Peptidyl Transferases Acyltransferases that use AMINO ACYL TRNA as the amino acid donor in formation of a peptide bond. There are ribosomal and non-ribosomal peptidyltransferases. Peptidyl Transferase,Peptidyl Translocase,Peptidyl Translocases,Peptidyltransferase,Transpeptidase,Transpeptidases,Peptidyltransferases,Transferase, Peptidyl,Transferases, Peptidyl,Translocase, Peptidyl,Translocases, Peptidyl
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D011550 Pseudomonas aeruginosa A species of gram-negative, aerobic, rod-shaped bacteria commonly isolated from clinical specimens (wound, burn, and urinary tract infections). It is also found widely distributed in soil and water. P. aeruginosa is a major agent of nosocomial infection. Bacillus aeruginosus,Bacillus pyocyaneus,Bacterium aeruginosum,Bacterium pyocyaneum,Micrococcus pyocyaneus,Pseudomonas polycolor,Pseudomonas pyocyanea
D002267 Muramoylpentapeptide Carboxypeptidase Enzyme which catalyzes the peptide cross-linking of nascent CELL WALL; PEPTIDOGLYCAN. Carboxypeptidase Transpeptidase,Carboxypeptidase, Muramoylpentapeptide,Transpeptidase, Carboxypeptidase
D002352 Carrier Proteins Proteins that bind or transport specific substances in the blood, within the cell, or across cell membranes. Binding Proteins,Carrier Protein,Transport Protein,Transport Proteins,Binding Protein,Protein, Carrier,Proteins, Carrier
D002437 Cefazolin A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial cell wall synthesis. It attains high serum levels and is excreted quickly via the urine. Cephazolin,Ancef,Cefamedin,Cefamezine,Cefazolin Sodium,Cephamezine,Cephazolin Sodium,Gramaxin,Kefzol,Sodium Cephazolin,Totacef,Cephazolin, Sodium,Sodium, Cefazolin,Sodium, Cephazolin
D002439 Cefotaxime Semisynthetic broad-spectrum cephalosporin. Benaxima,Biosint,Cefotaxim,Cefotaxime Sodium,Cefradil,Cephotaxim,Claforan,Fotexina,HR-756,Kendrick,Klaforan,Primafen,Ru-24756,Taporin,HR 756,HR756,Ru 24756,Ru24756,Sodium, Cefotaxime
D002441 Cefsulodin A pyridinium-substituted semisynthetic, broad-spectrum antibacterial used especially for Pseudomonas infections in debilitated patients. Abbott 46811,CGP-7174-E,Cefsulodin Monosodium Salt,Cefsulodin Sodium,Monaspor,Pyocefal,SCE-129,CGP 7174 E,CGP7174E,Monosodium Salt, Cefsulodin,SCE 129,SCE129,Sodium, Cefsulodin
D002442 Ceftazidime Semisynthetic, broad-spectrum antibacterial derived from CEPHALORIDINE and used especially for Pseudomonas and other gram-negative infections in debilitated patients. Ceftazidime Anhydrous,Ceftazidime Pentahydrate,Fortaz,Fortum,GR-20263,LY-139381,Pyridinium, 1-((7-(((2-amino-4-thiazolyl)((1-carboxy-1-methylethoxy)imino)acetyl)amino)-2-carboxy-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-en-3-yl)methyl)-, inner salt, pentahydrate, (6R-(6alpha,7beta(Z)))-,Tazidime,GR 20263,GR20263,LY 139381,LY139381

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