YAMADA H, HISADA H, MITSUYAMA M, TAKAHATA M, TODO Y, MINAMI S, TERASHIMA N, WATANABE Y, NARITA H; Interscience Conference on Antimicrobial Agents and Chemotherapy.
Abstr Intersci Conf Antimicrob Agents Chemother Intersci Conf Antimicrob Agents Chemother. 2000 Sep 17-20; 40: 82.
Res. laboratories, Toyama Chemical Co., Ltd., Toyama, Japan
T-3811ME, a des-F (6)-quinolone, exhibits a potent antibacterial activity against gram-positive cocci (PRSP, MRSA etc.). Many quinolones developed in recent decades are F (6)-quinolones (fluoroquinolones), and show bactericidal activity by inhibiting bacterial type II DNA topoisomerases (Topo). In this study, we determined inhibitory activities of T-3811ME, its F (6) derivative, and 3 fluoroquinolones against Topo IV and Gyr of S. pneumoniae, a major respiratory pathogen, and human Topo II from placenta. The inhibitory activities of T-3811ME against bacterial Topo (Topo IV and Gyr) were slightly inferior to those of the F (6) derivative but superior to those of other fluoroquinolones. Against human Topo II, the inhibitory activity of T-3811ME was weaker than that of the F (6) derivative and other fluoroquinolones. In conclusion, T-3811ME, a des-F (6)-quinolone, provides high selectivity (IC[50] against human Topo II (C)/IC[50] against Topo IV (A) or Gyr (B) of S. pneumoniae), while retaining enhanced antibacterial activity [table: see text]. Method: b: IC[50] showed 50% inhibitory activities of compounds against Topo. The activities of Topo IV, Gyr and Topo II were exhibited by decatenation, supercoiling, relaxation, respectively.KEYWORDS: Quinolones; Selectivity; Topoisomerase
Publication Types:
Keywords:
- Animals
- CASP4 protein, human
- Caspases
- DNA Topoisomerase IV
- DNA Topoisomerases, Type II
- DNA Topoisomerases, Type II, Bacterial
- Fluoroquinolones
- Humans
- Quinolones
- garenoxacin
Other ID:
UI: 102247572
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