Abstract
PD 138312 and PD 140248 are new quinolones with high in vitro activities against a wide spectrum of bacterial species, notably including gram-positive isolates. The respective MICs (in micrograms per milliliter) of PD 138312 and PD 140248 capable of inhibiting > or = 90% of the strains were < or = 0.06 and < or = 0.06 for oxacillin-susceptible and -resistant staphylococci, streptococci (including Streptococcus pyogenes, S. agalactiae, S. pneumoniae, and viridans group streptococci), Haemophilus influenzae, Moraxella catarrhalis, and Neisseria gonorrhoeae; 0.125 and 0.03 for Legionella pneumophila; 0.25 and 0.125 for Listeria monocytogenes; 0.25 and 0.25 for Enterococcus faecalis; 0.5 and 0.06 for anaerobic gram-positive cocci; 0.5 and 0.25 for Acinetobacter spp.; 0.5 and 0.5 for members of the family Enterobacteriaceae (excluding Serratia marcescens); 2 and 0.5 for Bacteroides fragilis; 2 and 2 for Serratia marcescens and ciprofloxacin-resistant staphylococci; and 8 and 4 for Pseudomonas aeruginosa.
Full text
PDF







Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Collins L. A., Malanoski G. J., Eliopoulos G. M., Wennersten C. B., Ferraro M. J., Moellering R. C., Jr In vitro activity of RP59500, an injectable streptogramin antibiotic, against vancomycin-resistant gram-positive organisms. Antimicrob Agents Chemother. 1993 Mar;37(3):598–601. doi: 10.1128/aac.37.3.598. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Domagala J. M., Hagen S. E., Joannides T., Kiely J. S., Laborde E., Schroeder M. C., Sesnie J. A., Shapiro M. A., Suto M. J., Vanderroest S. Quinolone antibacterials containing the new 7-[3-(1-aminoethyl)-1- pyrrolidinyl] side chain: the effects of the 1-aminoethyl moiety and its stereochemical configurations on potency and in vivo efficacy. J Med Chem. 1993 Apr 2;36(7):871–882. doi: 10.1021/jm00059a012. [DOI] [PubMed] [Google Scholar]
- Domagala J. M., Hanna L. D., Heifetz C. L., Hutt M. P., Mich T. F., Sanchez J. P., Solomon M. New structure-activity relationships of the quinolone antibacterials using the target enzyme. The development and application of a DNA gyrase assay. J Med Chem. 1986 Mar;29(3):394–404. doi: 10.1021/jm00153a015. [DOI] [PubMed] [Google Scholar]
- Edelstein P. H., Edelstein M. A., Weidenfeld J., Dorr M. B. In vitro activity of sparfloxacin (CI-978; AT-4140) for clinical Legionella isolates, pharmacokinetics in guinea pigs, and use to treat guinea pigs with L. pneumophila pneumonia. Antimicrob Agents Chemother. 1990 Nov;34(11):2122–2127. doi: 10.1128/aac.34.11.2122. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Lee B. L., Padula A. M., Kimbrough R. C., Jones S. R., Chaisson R. E., Mills J., Sande M. A. Infectious complications with respiratory pathogens despite ciprofloxacin therapy. N Engl J Med. 1991 Aug 15;325(7):520–521. doi: 10.1056/nejm199108153250719. [DOI] [PubMed] [Google Scholar]
- Maple P., Brumfitt W., Hamilton-Miller J. M. A review of the antimicrobial activity of the fluoroquinolones. J Chemother. 1990 Oct;2(5):280–294. doi: 10.1080/1120009x.1990.11739031. [DOI] [PubMed] [Google Scholar]
- Raviglione M. C., Boyle J. F., Mariuz P., Pablos-Mendez A., Cortes H., Merlo A. Ciprofloxacin-resistant methicillin-resistant Staphylococcus aureus in an acute-care hospital. Antimicrob Agents Chemother. 1990 Nov;34(11):2050–2054. doi: 10.1128/aac.34.11.2050. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Sanchez J. P., Domagala J. M., Hagen S. E., Heifetz C. L., Hutt M. P., Nichols J. B., Trehan A. K. Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinoline-3-carboxylic acids and 1,8-naphthyridine-3-carboxylic acids. J Med Chem. 1988 May;31(5):983–991. doi: 10.1021/jm00400a016. [DOI] [PubMed] [Google Scholar]
- Shalit I., Berger S. A., Gorea A., Frimerman H. Widespread quinolone resistance among methicillin-resistant Staphylococcus aureus isolates in a general hospital. Antimicrob Agents Chemother. 1989 Apr;33(4):593–594. doi: 10.1128/aac.33.4.593. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Shapiro M. A., Heifetz C. L., Sesnie J. C. Comparison of microdilution and agar dilution procedures for testing antibiotic susceptibility of Neisseria gonorrhoeae. J Clin Microbiol. 1984 Oct;20(4):828–830. doi: 10.1128/jcm.20.4.828-830.1984. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Wolfson J. S., Hooper D. C. Fluoroquinolone antimicrobial agents. Clin Microbiol Rev. 1989 Oct;2(4):378–424. doi: 10.1128/cmr.2.4.378. [DOI] [PMC free article] [PubMed] [Google Scholar]