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JAC Advance Access published online on July 27, 2006
Journal of Antimicrobial Chemotherapy, doi:10.1093/jac/dkl304
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© The Author 2006. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions@oxfordjournals.org
Received January 8, 2006
Revised June 26, 2006
Accepted July 4, 2006

Original article

In vitro and in vivo activities of DW-224a, a novel fluoroquinolone antibiotic agent

Ae-Ran Kwon 1, Yu-Hong Min 1, Jei-Man Ryu 2, Dong-Rack Choi 2, Mi-Ja Shim 3, and Eung-Chil Choi 1 *

1 College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Korea
2 Dong-Wha Pharmaceutical Ind. Co., Ltd, Anyang, Gyunggi 430-017, Korea
3 Department of Life Science, The University of Seoul, Seoul 130-743, Korea

* To whom correspondence should be addressed.
Eung-Chil Choi, E-mail: ecchoi{at}snu.ac.kr


  Abstract

Objectives: The objective of the present study was to assess the in vitro and in vivo activities of DW-224a in order to eventually use it as an antibiotic.

Methods: DW-224a was compared with DW286, ciprofloxacin and trovafloxacin. MICs of DW-224a, DW286, ciprofloxacin and trovafloxacin were determined against several groups of clinical isolates. In addition, intraperitoneal infection was induced with various organisms in mice. Test compounds were administered once orally to mice immediately after infection. The 50% protective dose (PD50) was calculated from the survival rates on day 7 after infection.

Results: Against Gram-positive bacteria, the in vitro activity of DW-224a was stronger than those of ciprofloxacin and trovafloxacin, but slightly weaker than that of DW286. Against Gram-negative bacteria, the activity of DW-224a was similar to those of trovafloxacin and DW286, but weaker than that of ciprofloxacin. In experimental systemic infections in mice with various organisms, like DW286, DW-224a demonstrated potent activity against Gram-positive bacteria and somewhat less activity against Gram-negative bacteria.

Conclusions: DW-224a has a broad spectrum of antimicrobial activity, which is especially potent against Gram-positive bacteria.

Keywords: ciprofloxacin; trovafloxacin; DW286; MICs; PD50.
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