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In vitro and in vivo antimicrobial activities of T-3811ME, a novel des-F(6)-quinolone.

Abstract
The in vitro and in vivo activities of T-3811ME, a novel des-F(6)-quinolone, were evaluated in comparison with those of some fluoroquinolones, including a newly developed one, trovafloxacin. T-3811, a free base of T-3811ME, showed a wide range of antimicrobial spectra, including activities against Chlamydia trachomatis, Mycoplasma pneumoniae, and Mycobacterium tuberculosis. In particular, T-3811 exhibited potent activity against various gram-positive cocci, with MICs at which 90% of the isolates are inhibited (MIC90s) of 0.025 to 6.25 microgram/ml. T-3811 was the most active agent against methicillin-resistant Staphylococcus aureus and streptococci, including penicillin-resistant Streptococcus pneumoniae (PRSP). T-3811 also showed potent activity against quinolone-resistant gram-positive cocci with GyrA and ParC (GrlA) mutations. The activity of T-3811 against members of the family Enterobacteriaceae and nonfermentative gram-negative rods was comparable to that of trovafloxacin. In common with other fluoroquinolones, T-3811 was highly active against Haemophilus influenzae, Moraxella catarrhalis, and Legionella sp., with MIC90s of 0.0125 to 0.1 microgram/ml. T-3811 showed a potent activity against anaerobic bacteria, such as Bacteroides fragilis and Clostridium difficile. T-3811 was the most active agent against C. trachomatis (MIC, 0.008 microgram/ml) and M. pneumoniae (MIC90, 0.0313 microgram/ml). The activity of T-3811 against M. tuberculosis (MIC90, 0.0625 microgram/ml) was potent and superior to that of trovafloxacin. In experimental systemic infection with a GrlA mutant of S. aureus and experimental pneumonia with PRSP in mice, T-3811ME showed excellent therapeutic efficacy in oral and subcutaneous administrations.
AuthorsM Takahata, J Mitsuyama, Y Yamashiro, M Yonezawa, H Araki, Y Todo, S Minami, Y Watanabe, H Narita
JournalAntimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 43 Issue 5 Pg. 1077-84 (May 1999) ISSN: 0066-4804 [Print] United States
PMID10223917 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Anti-Infective Agents
  • Fluoroquinolones
  • Indoles
  • Isoindoles
  • Naphthyridines
  • Quinolones
  • T 3811ME
  • Ciprofloxacin
  • trovafloxacin
  • Ofloxacin
Topics
  • Administration, Oral
  • Animals
  • Anti-Infective Agents (administration & dosage, pharmacology, therapeutic use)
  • Bacteria (drug effects)
  • Bacterial Infections (drug therapy)
  • Ciprofloxacin (pharmacology)
  • Fluoroquinolones
  • Indoles (administration & dosage, therapeutic use)
  • Injections, Subcutaneous
  • Isoindoles
  • Male
  • Mice
  • Naphthyridines (pharmacology)
  • Ofloxacin (pharmacology)
  • Quinolones (administration & dosage, therapeutic use)

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