In vitro activity of enoxacin, a quinolone carboxylic acid, compared with those of norfloxacin, new beta-lactams, aminoglycosides, and trimethoprim

Abstract

Enoxacin is a new quinolone carboxylic acid compound. Its activity against 740 bacterial isolates was determined. It inhibited 90% Escherichia coli, Klebsiella sp., Aeromonas sp., Enterobacter spp., Serratia spp., Proteus mirabilis, and Morganella morganii at -0.8 ,ug/ml. The majority of Pseudomonas aeruginosa was inhibited by <3.1 p.g/ml. Haemophilus spp. and Neisseria spp. were inhibited by <0.1 jig/ml. Although most Staphylococcus aureus were inhibited by 3.1 ,ug/ml, some streptococcal species had minimal inhibitory concentrations of 6.3 to 12.5 ,ug/ml and Bacteroides sp. had minimal inhibitory concentrations -25 ,ug/ml. Activity of enoxacin and norfloxacin was similar. Enoxacin inhibited organisms resistant to cefotaxime, moxalactam, gentamicin, and piperacillin. Enoxacin was less active in urine at an acid pH than in broth, but serum did not decrease minimal inhibitory concentrations or minimal bactericidal concentrations. There was no major difference between minimal inhibitory concentrations and minimal bactericidal concentrations. Resistance frequency development was <10-9 for most bacterial species.Quinolone antimicrobial agents such as nalidixic acid and related compounds have been used primarily to treat urinary tract infections. Agents of this class have various ring structures affixed to y-pyridone-p-carboxylic acid which appears to be essential for the activity of these synthetic compounds. Recently, compounds have been synthesized which do not appear to suffer from the defects of nalidixic acid, namely restricted antibacterial activity and poor oral absorption. These agents are active against bacteria resistant to nalidixic acid, and they inhibit gram-positive species and Pseudomonas aeruginosa (4, 7). Enoxacin, formerly called AT-2266 or CI 919, is a 1-ethyl-6-fluro-1,4-dihydro-4-oxa-7-(1-piperazinyl)-

Enoxacin Directly Inhibits Osteoclastogenesis without Inducing Apoptosis

“…Macrophage colonystimulating factor (CSF-1) was obtained from Peprotech. Enoxacin was obtained from Sigma-Aldrich and dissolved in DMSO (1) or 0.1 M sodium hydroxide (32).…”

A pleiotropic, posttherapy, enoxacin-resistant mutant of Pseudomonas aeruginosa

“…One of these revertants was characterized in more detail and shown to be indistinguishable in all properties from the pretherapy isolate. It is proposed that the multiple-antibiotic-resistance (Mar) phenotype of this mutant resulted from a single pleiotropic mutation.Enoxacin is a difluorinated quinolone with strong activity for gram-negative bacteria (7,41). Enoxacin is now marketed in 11 countries, including South America, the United Kingdom, and other parts of Europe, for use in the therapy of urinary tract infections and in some countries for respiratory tract infections.…”

“…Enoxacin is a difluorinated quinolone with strong activity for gram-negative bacteria (7,41). Enoxacin is now marketed in 11 countries, including South America, the United Kingdom, and other parts of Europe, for use in the therapy of urinary tract infections and in some countries for respiratory tract infections.…”

New Improved Quinlone Derivatives Against Infection

“…Generally, the 7-piperazinyl enoxacin have better Gram-negative than Gram-positive antimicrobial potency (Chin & Neu, 1983, Paton & Reeves, 1988, Wood, 1989. Studies revealed that the mode of action of quinolones involves inhibition of essential type II bacterial topoisomerases such as DNA gyrase and topoisomerase IV (Sissi & Palumbo, 2003).…”