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Antimicrobial Agents and Chemotherapy, May 1999, p. 1077-1084, Vol. 43, No. 5
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.

In Vitro and In Vivo Antimicrobial Activities of T-3811ME, a Novel Des-F(6)-Quinolone

Masahiro Takahata,* Junichi Mitsuyama, Yoshiko Yamashiro, Minoru Yonezawa, Harumi Araki, Yozo Todo, Shinzaburo Minami, Yasuo Watanabe, and Hirokazu Narita

Research Laboratories, Toyama Chemical Co., Ltd., Toyama, Japan

Received 9 November 1998/Returned for modification 22 January 1999/Accepted 5 March 1999

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 µg/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 µg/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 µg/ml) and M. pneumoniae (MIC90, 0.0313 µg/ml). The activity of T-3811 against M. tuberculosis (MIC90, 0.0625 µg/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.

* Corresponding author. Mailing address: Research Laboratories, Toyama Chemical Co., Ltd., 4-1, Shimookui 2-chome, Toyama 930-8508, Japan. Phone: 81-764-31-8268. Fax: 81-764-31-8208. E-mail: takahata{at}labo.toyama-chemical.co.jp.

Antimicrobial Agents and Chemotherapy, May 1999, p. 1077-1084, Vol. 43, No. 5
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.


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