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Chemical Compound Review

Ozex     7-(3-aminopyrrolidin-1-yl)-1- (2,4...

Synonyms: TFLX, Tosufloxacin, Abbott-61827, SureCN34354, AGN-PC-00C1LC, ...
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Disease relevance of Tosufloxacin


High impact information on Tosufloxacin


Chemical compound and disease context of Tosufloxacin


Biological context of Tosufloxacin


Anatomical context of Tosufloxacin


Associations of Tosufloxacin with other chemical compounds


Gene context of Tosufloxacin

  • These results suggest that tosufloxacin may delay neutrophil apoptosis via activation of PI3K/Akt and/or p38 MAPK, and the other quinolones may promote neutrophil death without affecting their apoptosis [13].
  • For the parC mutant strain D-3197, both the AUC(0-24h)/MIC and C(max)/MIC ratios of tosufloxacin were greater than those of levofloxacin, which resulted in comparable or better bactericidal activity as compared to those of levofloxacin [21].
  • Tosufloxacin, a new quinolone, had very good activity against B. fragilis group strains (94% susceptible), good activity against other beta-lactamase-positive strains (less than or equal 85% susceptible), and excellent activity against beta-lactamase-negative strains (100% susceptible; MIC for 90% of strains, 0.5 microgram/ml) [22].
  • IC50s of levofloxacin, ciprofloxacin, sparfloxacin and tosufloxacin against DNA gyrase were almost three to 12 times higher than those against topoisomerase IV [23].
  • Despite administration of antibiotics (piperacillin sodium, PIPC; and tosufloxacin tosilate, TFLX), fever and an elevation of the c-reactive protein (CRP) level with neutrophilia appeared, and an infiltration shadow was observed in the right lower pulmonary field [24].

Analytical, diagnostic and therapeutic context of Tosufloxacin


  1. In vitro activity of tosufloxacin, a new quinolone, against respiratory pathogens derived from cystic fibrosis sputum. Arguedas, A.G., Akaniro, J.C., Stutman, H.R., Marks, M.I. Antimicrob. Agents Chemother. (1990) [Pubmed]
  2. Intracellular activity of tosufloxacin (T-3262) against Salmonella enteritidis and ability to penetrate into tissue culture cells of human origin. Noumi, T., Nishida, N., Minami, S., Watanabe, Y., Yasuda, T. Antimicrob. Agents Chemother. (1990) [Pubmed]
  3. A-61827 (A-60969), a new fluoronaphthyridine with activity against both aerobic and anaerobic bacteria. Fernandes, P.B., Chu, D.T., Swanson, R.N., Ramer, N.R., Hanson, C.W., Bower, R.R., Stamm, J.M., Hardy, D.J. Antimicrob. Agents Chemother. (1988) [Pubmed]
  4. In vitro and in vivo antibacterial activities of CS-940, a new fluoroquinolone, against isolates from patients with respiratory infections. Miyazaki, S., Domon, H., Tateda, K., Ohno, A., Ishii, Y., Matsumoto, T., Furuya, N., Yamaguchi, K. Antimicrob. Agents Chemother. (1997) [Pubmed]
  5. Antibacterial activities and pharmacokinetics of E-4767 and E-5065, two new 8-chlorofluoroquinolones with a 7-azetidin ring substituent. Gargallo-Viola, D., Ferrer, S., Tudela, E., Robert, M., Coll, R., Roser, R., Guinea, J. Antimicrob. Agents Chemother. (2001) [Pubmed]
  6. In vitro and in vivo activities of sitafloxacin against Chlamydia spp. Miyashita, N., Niki, Y., Matsushima, T. Antimicrob. Agents Chemother. (2001) [Pubmed]
  7. Salmonella excretion after cessation of tosufloxacin therapy in acute nontyphoid salmonella enterocolitis. Ohnishi, K., Kimura, K. Antimicrob. Agents Chemother. (2001) [Pubmed]
  8. Effects of aluminum hydroxide and famotidine on bioavailability of tosufloxacin in healthy volunteers. Minami, R., Nakamura, C., Inotsume, N., Nakano, M. Antimicrob. Agents Chemother. (1998) [Pubmed]
  9. In vitro and in vivo antichlamydial activities of newly developed quinolone antimicrobial agents. Kimura, M., Kishimoto, T., Niki, Y., Soejima, R. Antimicrob. Agents Chemother. (1993) [Pubmed]
  10. Comparative in-vitro and in-vivo activity of AM-1155 against anaerobic bacteria. Kato, N., Kato, H., Tanaka-Bandoh, K., Watanabe, K., Ueno, K. J. Antimicrob. Chemother. (1997) [Pubmed]
  11. In vitro activity of pazufloxacin, tosufloxacin and other quinolones against Legionella species. Higa, F., Akamine, M., Haranaga, S., Tohyama, M., Shinzato, T., Tateyama, M., Koide, M., Saito, A., Fujita, J. J. Antimicrob. Chemother. (2005) [Pubmed]
  12. In-vitro activity of tosufloxacin, a new quinolone antibacterial agent. Cooper, M.A., Andrews, J.M., Wise, R. J. Antimicrob. Chemother. (1992) [Pubmed]
  13. Alteration of constitutive apoptosis in neutrophils by quinolones. Azuma, Y., Ohura, K. Inflammation (2003) [Pubmed]
  14. Stereoselective analysis of the disposition of tosufloxacin enantiomers in man. Minami, R., Inotsume, N., Nakamura, C., Nakano, M. Eur. J. Clin. Pharmacol. (1993) [Pubmed]
  15. Antibacterial activities of tosufloxacin against anaerobic bacteria and the electron micrograph of its bactericidal effects. Takahata, M., Nishino, T. Chemotherapy. (1997) [Pubmed]
  16. Therapeutic effect of the quinolone prodrug prulifloxacin against experimental urinary tract infections in mice. Tomii, Y., Ozaki, M., Matsuda, M., Honmura, T., Nishimura, I., Yamaguchi, R., Adachi, T., Okawa, Y., Nishino, T. Arzneimittel-Forschung. (1996) [Pubmed]
  17. Quinolones alter defense reactions mediated by macrophages. Azuma, Y., Shinohara, M., Wang, P.L., Ohura, K. Int. Immunopharmacol. (2001) [Pubmed]
  18. In vitro and in vivo antibacterial activities of a new quinolone, OPC-17116. Imada, T., Miyazaki, S., Nishida, M., Yamaguchi, K., Goto, S. Antimicrob. Agents Chemother. (1992) [Pubmed]
  19. In vitro activity of tosufloxacin (A-61827; T-3262) against selected genital pathogens. Segreti, J., Hirsch, D.J., Harris, A.A., Kapell, K.S., Orbach, H., Kessler, H.A. Antimicrob. Agents Chemother. (1990) [Pubmed]
  20. In-vitro activities of temafloxacin, tosufloxacin (A-61827) and five other fluoroquinolone agents. Barry, A.L., Jones, R.N. J. Antimicrob. Chemother. (1989) [Pubmed]
  21. Pharmacodynamic evaluation of tosufloxacin against Streptococcus pneumoniae in an in vitro model simulating serum concentration. Fukuda, Y., Takahata, M., Mitsuyama, J. J. Infect. Chemother. (2006) [Pubmed]
  22. Susceptibilities of 394 Bacteroides fragilis, non-B. fragilis group Bacteroides species, and Fusobacterium species to newer antimicrobial agents. Appelbaum, P.C., Spangler, S.K., Jacobs, M.R. Antimicrob. Agents Chemother. (1991) [Pubmed]
  23. Dual inhibitory activity of sitafloxacin (DU-6859a) against DNA gyrase and topoisomerase IV of Streptococcus pneumoniae. Onodera, Y., Uchida, Y., Tanaka, M., Sato, K. J. Antimicrob. Chemother. (1999) [Pubmed]
  24. Pulmonary infiltration with eosinophilia (PIE) syndrome induced by antibiotics, PIPC and TFLX during cancer treatment. Yamamoto, T., Tanida, T., Ueta, E., Kimura, T., Doi, S., Osaki, T. Oral Oncol. (2001) [Pubmed]
  25. Susceptibility of anaerobic bacteria to tosufloxacin. Nord, C.E., Lindmark, A., Persson, I., Runow, C. Eur. J. Clin. Microbiol. Infect. Dis. (1992) [Pubmed]
  26. Sensitivity of Staphylococcus aureus, isolated from skin infections in 1994, to 19 antimicrobial agents. Nishijima, S., Nakagawa, M., Sugiyama, T., Akamatsu, H., Horio, T., Kawabata, S., Fujita, M. J. Int. Med. Res. (1995) [Pubmed]
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