| pubmed-article:7726507 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:7726507 | lifeskim:mentions | umls-concept:C1707919 | lld:lifeskim |
| pubmed-article:7726507 | lifeskim:mentions | umls-concept:C0450254 | lld:lifeskim |
| pubmed-article:7726507 | lifeskim:mentions | umls-concept:C0172670 | lld:lifeskim |
| pubmed-article:7726507 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:7726507 | pubmed:dateCreated | 1995-5-23 | lld:pubmed |
| pubmed-article:7726507 | pubmed:abstractText | E-4695, (-)-7-[3-(R)-amino-2-(S)-methyl-1-azetidinyl]-1-cyclopropyl-1,4- dihydro-6-fluoro-4-oxo-1,8-naphthyridine-3-carboxylic acid, is a new fluorinated naphthyridine with an azetidine moiety. The MICs of E-4695 at which 90% of the isolates were inhibited (MIC90s) were 0.06 to 0.5 microgram/ml for gram-positive cocci, including species of the genera Staphylococcus, Streptococcus, and Enterococcus, and the MIC90s against gram-negative pathogens such as members of the family Enterobacteriaceae (with the exception of Providencia spp. [MIC90, 8 micrograms/ml]) and Pseudomonas aeruginosa were 0.015 to 0.5 microgram/ml. E-4695 inhibited 90% of the Clostridium perfringens and Bacteroides fragilis isolates at 0.25 and 4 micrograms/ml, respectively. Against gram-positive cocci the potency of E-4695 was 2- to 8-fold higher than that of ciprofloxacin, 4- to 8-fold higher than that of ofloxacin, and 8- to 16-fold higher than that of fleroxacin. Against enteric bacteria and P. aeruginosa the potency of E-4695 was, in general, similar to that of ciprofloxacin and eightfold higher than those of ofloxacin and fleroxacin. E-4695 was four- and eightfold more potent than ciprofloxacin against C. perfringens and B. fragilis isolates, respectively. E-4695 and ciprofloxacin showed similar properties when the effects of pH or magnesium concentration were tested on them. E-4695 and ciprofloxacin had substantial reductions of activity only when pH decreased below 4.8. E-4695 and ciprofloxacin activities were not markedly affected by the presence of 5 or 10 mM Mg2+. The presence of serum and human urine at pH 7.2 decreased the activity of E-4695 between two- and fourfold. After an oral dose of 50 mg/kg of body weight, the maximum level in serum, the biological half-life, and the area under the concentration-time curve from 0 to 10 h for E-4695 were 13.2 microgram/ml, 3.3 h, and 45.6 microgram . h/ml, respectively. The area under the concentration-time curve from 0 to 4 h for ciprofloxacin was 2.3 microgram . h/ml at the same dose. Fifty-percent effective doses (ED50S) against Staphylococcus aureus HS-93 infections in mice were 4.5 mg/kg with E-4695 and 37.6 mg/kg with ciprofloxacin. Infection with Streptococcus pneumoniae 29206 was more effectively treated with E-4695 (ED50, 41,2 mg/kg) than with ciprofloxacin (ED50, 200 mg/kg). The ED50 of E-4695 for infections with Streptococcus pneumoniae 1625 was 132.2 mg/kg; ciprofloxacin was ineffective at 400 mg/kg against this strain. E-4695 was also more potent than ciprofloxacin in treatment of infections caused by gram-negative organisms such as Escherichia coli HM-42 (ED50S, 1.0 and 3.9 mg/kg, respectively). The ED50S of E-4695 and ciprofloxacin were 33.0 and 145.5 mg/kg against P. aeruginosa HS-116 and 9.6 and 18.9 mg/kg against P. aeruginosa B-120, respectively. The therapeutic efficacy of E-4695 may depend not only on its in vitro activity but also on its improved pharmacokinetic properties. | lld:pubmed |
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| pubmed-article:7726507 | pubmed:language | eng | lld:pubmed |
| pubmed-article:7726507 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:7726507 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:7726507 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:7726507 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:7726507 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:7726507 | pubmed:month | Feb | lld:pubmed |
| pubmed-article:7726507 | pubmed:issn | 0066-4804 | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:RobertMM | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:GarciaJJ | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:CollRR | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:RoserRR | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:GuineaJJ | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:EsteveMM | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:Gargallo-Viol... | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:XicotaM AMA | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:TudelaEE | lld:pubmed |
| pubmed-article:7726507 | pubmed:author | pubmed-author:ParesMM | lld:pubmed |
| pubmed-article:7726507 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:7726507 | pubmed:volume | 39 | lld:pubmed |
| pubmed-article:7726507 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:7726507 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:7726507 | pubmed:pagination | 413-21 | lld:pubmed |
| pubmed-article:7726507 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
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| pubmed-article:7726507 | pubmed:meshHeading | pubmed-meshheading:7726507-... | lld:pubmed |
| pubmed-article:7726507 | pubmed:year | 1995 | lld:pubmed |
| pubmed-article:7726507 | pubmed:articleTitle | E-4695, a new C-7 azetidinyl fluoronaphthyridine with enhanced activity against gram-positive and anaerobic pathogens. | lld:pubmed |
| pubmed-article:7726507 | pubmed:affiliation | Department of Sanitary Microbiology and Parasitology, Faculty of Pharmacy, University of Barcelona, Spain. | lld:pubmed |
| pubmed-article:7726507 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:7726507 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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