Abstract
The in vitro antibacterial activity of AM-1155 against a wide variety of clinical isolates was compared with those of other fluoroquinolones. The MICs of AM-1155 for 90% of Staphylococcus aureus, Streptococcus pneumoniae, and Enterococcus faecalis isolates tested were 0.10, 0.39, and 0.78 microgram/ml, respectively. The antibacterial activity of AM-1155 against gram-positive bacteria and anaerobes was comparable to those of sparfloxacin and tosufloxacin. AM-1155 inhibited 90% of most species of the family Enterobacteriaceae at a concentration of 0.39 microgram/ml. AM-1155 generally had activity comparable to that of sparfloxacin against gram-negative bacteria. AM-1155 showed moderate activity against methicillin- and quinolone-resistant S. aureus. AM-1155 demonstrated bactericidal activity at the MIC. The frequency of occurrence of spontaneous mutants resistant to four times the MIC of AM-1155 was < 1 x 10(9) for S. aureus, Escherichia coli, and Pseudomonas aeruginosa. AM-1155 strongly inhibited the supercoiling activities of DNA gyrases purified from E. coli and S. aureus.
Full text
PDF







Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Aoyama H., Sato K., Fujii T., Fujimaki K., Inoue M., Mitsuhashi S. Purification of Citrobacter freundii DNA gyrase and inhibition by quinolones. Antimicrob Agents Chemother. 1988 Jan;32(1):104–109. doi: 10.1128/aac.32.1.104. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Crumplin G. C., Kenwright M., Hirst T. Investigations into the mechanism of action of the antibacterial agent norfloxacin. J Antimicrob Chemother. 1984 May;13 (Suppl B):9–23. doi: 10.1093/jac/13.suppl_b.9. [DOI] [PubMed] [Google Scholar]
- Fujimaki K., Noumi T., Saikawa I., Inoue M., Mitsuhashi S. In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone. Antimicrob Agents Chemother. 1988 Jun;32(6):827–833. doi: 10.1128/aac.32.6.827. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hane M. W., Wood T. H. Escherichia coli K-12 mutants resistant to nalidixic acid: genetic mapping and dominance studies. J Bacteriol. 1969 Jul;99(1):238–241. doi: 10.1128/jb.99.1.238-241.1969. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hirai K., Aoyama H., Hosaka M., Oomori Y., Niwata Y., Suzue S., Irikura T. In vitro and in vivo antibacterial activity of AM-833, a new quinolone derivative. Antimicrob Agents Chemother. 1986 Jun;29(6):1059–1066. doi: 10.1128/aac.29.6.1059. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hirose T., Okezaki E., Kato H., Ito Y., Inoue M., Mitsuhashi S. In vitro and in vivo activity of NY-198, a new difluorinated quinolone. Antimicrob Agents Chemother. 1987 Jun;31(6):854–859. doi: 10.1128/aac.31.6.854. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Hosaka M., Yasue T., Fukuda H., Tomizawa H., Aoyama H., Hirai K. In vitro and in vivo antibacterial activities of AM-1155, a new 6-fluoro-8-methoxy quinolone. Antimicrob Agents Chemother. 1992 Oct;36(10):2108–2117. doi: 10.1128/aac.36.10.2108. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Ito A., Hirai K., Inoue M., Koga H., Suzue S., Irikura T., Mitsuhashi S. In vitro antibacterial activity of AM-715, a new nalidixic acid analog. Antimicrob Agents Chemother. 1980 Feb;17(2):103–108. doi: 10.1128/aac.17.2.103. [DOI] [PMC free article] [PubMed] [Google Scholar]
- King A., Warren C., Shannon K., Phillips I. In vitro antibacterial activity of norfloxacin (MK-0366). Antimicrob Agents Chemother. 1982 Apr;21(4):604–607. doi: 10.1128/aac.21.4.604. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Kojima T., Inoue M., Mitsuhashi S. In vitro activity of AT-4140 against clinical bacterial isolates. Antimicrob Agents Chemother. 1989 Nov;33(11):1980–1988. doi: 10.1128/aac.33.11.1980. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Nakanishi N., Yoshida S., Wakebe H., Inoue M., Yamaguchi T., Mitsuhashi S. Mechanisms of clinical resistance to fluoroquinolones in Staphylococcus aureus. Antimicrob Agents Chemother. 1991 Dec;35(12):2562–2567. doi: 10.1128/aac.35.12.2562. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Neu H. C., Labthavikul P. In vitro activity of norfloxacin, a quinolinecarboxylic acid, compared with that of beta-lactams, aminoglycosides, and trimethoprim. Antimicrob Agents Chemother. 1982 Jul;22(1):23–27. doi: 10.1128/aac.22.1.23. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Neu H. C., Novelli A., Chin N. X. Comparative in vitro activity of a new quinolone, AM-1091. Antimicrob Agents Chemother. 1989 Jul;33(7):1036–1041. doi: 10.1128/aac.33.7.1036. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Sato K., Inoue Y., Fujii T., Aoyama H., Inoue M., Mitsuhashi S. Purification and properties of DNA gyrase from a fluoroquinolone-resistant strain of Escherichia coli. Antimicrob Agents Chemother. 1986 Nov;30(5):777–780. doi: 10.1128/aac.30.5.777. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Sato K., Matsuura Y., Inoue M., Une T., Osada Y., Ogawa H., Mitsuhashi S. In vitro and in vivo activity of DL-8280, a new oxazine derivative. Antimicrob Agents Chemother. 1982 Oct;22(4):548–553. doi: 10.1128/aac.22.4.548. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Traub W. H. Incomplete cross-resistance of nalidixic and pipemidic acid-resistant variants of Serratia marcescens against ciprofloxacin, enoxacin, and norfloxacin. Chemotherapy. 1985;31(1):34–39. doi: 10.1159/000238311. [DOI] [PubMed] [Google Scholar]
- Wise R., Andrews J. M., Edwards L. J. In vitro activity of Bay 09867, a new quinoline derivative, compared with those of other antimicrobial agents. Antimicrob Agents Chemother. 1983 Apr;23(4):559–564. doi: 10.1128/aac.23.4.559. [DOI] [PMC free article] [PubMed] [Google Scholar]