Currently available quinolones are either inactive or marginally active against anaerobic bacteria. This review summarises the in vitro activity of currently available as well as experimental quinolones against clinically significant anaerobic bacteria. Quinolones with low activity against anaerobes include ciprofloxacin, ofloxacin, levofloxacin, fleroxacin, pefloxacin, enoxacin, lomefloxacin and probably E 4868 and NM 441. Compounds with intermediate anaerobe activity include sparfloxacin, grepafloxacin, PD 131628 and AM 1155. Quinolones that are very active against anaerobes include clinafloxacin and DU 6859a. CP 99,219, a naphthyridone, is also very active against anaerobes. Toxicity problems have necessitated the withdrawal of some quinolones shown to have intermediate activity (temafloxacin and tosufloxacin) and the discontinuation of the development of some investigational agents (Win 57273 and BAY Y 3118) with high activity. Conclusions regarding the therapeutic value of quinolones against human anaerobic infections await further clinical toxicological and pharmacokinetic studies.

1995-01-01·Drugs under experimental and clinical research

In vitro activity of E-4868, a new fluoroquinolone with a 7-azetidin ring, compared with ciprofloxacin, ofloxacin and fleroxacin.

Article

作者: Prats, G ; Xicota, M A ; Coll, R ; Miró, E ; Mirelis, B ; Navarro, F

E-4868, (-)-7[3-(R)-amino-2-(S)-methyl-1-azetidinyl]-1-(2,4- difluorophenyl)-1,4-dihydro-6-fluoro-4-oxo-3-quinolinecarboxylic acid, is a new fluoroquinolone with a 7-azetidin ring substituent. The in vitro activity against clinical isolates was compared with that of ciprofloxacin, ofloxacin and fleroxacin. In general, activity of E-4868 against aerobic and facultative anaerobic Gram-negative bacilli was equal to or slightly less active than ciprofloxacin with the exception of Morganella morganii and Proteus spp., E-4868 MIC90, 1 and 0.5 microgram/ml, respectively. E-4868 activity was two- to eight-fold higher than ciprofloxacin against Gram-positive cocci. For anaerobic species, E-4868 activity was comparable to that of ciprofloxacin, although against the Bacteroides fragilis group E-4868 was four-fold more active than ciprofloxacin.

1994-06-01·Antimicrobial agents and chemotherapy2区 · 医学

Comparative in vitro activities of new quinolones against coryneform bacteria

2区 · 医学

Article

作者: Ortega, M C ; Perea, E J ; Martínez-Martínez, L ; Suárez, A I

The in vitro activities of eight quinolones against 115 coryneform bacteria (20 Corynebacterium jeikeium, 15 Corynebacterium minutissimum, 15 Corynebacterium striatum, 25 Corynebacterium urealyticum, 10 Corynebacterium xerosis, 10 Corynebacterium group ANF-1, 10 Corynebacterium group 12, and 10 Listeria monocytogenes) were determined. The MICs of ciprofloxacin, ofloxacin, and sparfloxacin for 90% of C. jeikeium, C. urealyticum, and C. xerosis isolates tested were > 16 micrograms/ml. Those of BAY Y 3118 and clinafloxacin against these species were 0.5 and 1 to 2 micrograms/ml, respectively. The MICs for 90% of all 115 strains tested were 0.5 microgram/ml for BAY Y 3118, 1 microgram/ml for clinafloxacin, 2 micrograms/ml for E-5068, 4 micrograms/ml for E-5065, and > 16 micrograms/ml for ciprofloxacin, ofloxacin, sparfloxacin, and E-4868.

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