Fluoroquinolone resistance of Streptococcus pneumoniae isolates causing invasive disease: special focus on zabofloxacin.

The present study examined the in vitro activity of various antibiotics including zabofloxacin, against isolates responsible for invasive pneumococcal diseases. Between 1997 and 2008, a total of 208 isolates were collected from sterile fluids, including blood (n=196, 94.2%), pleural fluid (n=5, 2.

Antimicrobial activity of DW286 against Streptococcus pneumoniae.

DW286 is a novel broad-spectrum fluoroquinolone with excellent antipneumococcal activity. The in vitro activity of DW286 was evaluated against quinolone-susceptible and -resistant Streptococcus pneumoniae and was compared with the activities of reference compounds. Among the tested agents, DW286 showed the most potent antibacterial activity against 94 quinolone-susceptible strains [minimum inhibitory concentration (MIC) 0.

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

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 vitro and in vivo antibacterial activities of DW-224a, a new fluoronaphthyridone.

DW-224a showed the most potent in vitro activity among the quinolone compounds tested against clinical isolates of gram-positive bacteria. Against gram-negative bacteria, DW-224a was slightly less active than the other fluoroquinolones. The in vivo activities of DW-224a against gram-positive bacteria were more potent than those of other quinolones.

Antipneumococcal activity of DW-224a, a new quinolone, compared to those of eight other agents.

DW-224a is a new broad-spectrum quinolone with excellent antipneumococcal activity. Agar dilution MIC was used to test the activity of DW-224a compared to those of penicillin, ciprofloxacin, levofloxacin, gatifloxacin, moxifloxacin, gemifloxacin, amoxicillin-clavulanate, cefuroxime, and azithromycin against 353 quinolone-susceptible pneumococci. The MICs of 29 quinolone-resistant pneumococci with defined quinolone resistance mechanisms against seven quinolones and an efflux mechanism were also tested.

Diastereoselective synthesis of polysubstituted pyrrolidinone as a key intermediate for the anticancer agents by palladium(II)-catalyzed carboxylation.

Palladium(II)-catalyzed carboxylation of chiral olefins 6a-d has been examined under various conditions. In the weak basic condition (K2CO3), 7a-d were obtained in good yields. Alternatively, in the strong basic condition, pyrrolidinones 8a-d were obtained resulting in excellent yields and with high diastereoselectivity.

Synthesis and cytotoxic activity of 1-(1-benzoylindoline-5-sulfonyl)-4-phenylimidazolidinones.

The novel 1-(1-benzoylindoline-5-sulfonyl)-4-phenyl-4,5-dihydroimidazolones 2 shows highly potent and broad cytotoxicities. Their cytotoxicities against human lung carcinoma A549, human chronic myelogenous leukemia K562, and human ovarian adenocarcinoma SK-OV-3 are compatible with doxorubicin. Compound 2p (1-[(4-aminobenzoyl)indoline-5-sulfonyl])-4-phenyl-4,5-dihydroimidazolone) exhibits a cytotoxicity that is far more potent than doxorubicin and also exhibits highly effective antitumour activities against murine (3LL, Colon 26) and human xenograft (NCI-H23, SW620) tumor models.

Syntheses and biological evaluation of new fluoroquinolone antibacterials containing chiral oxiimino pyrrolidine.

The design and syntheses of new fluoroquinolone antibacterial agents having pyrrolidine ring at C-7 position are described. The pyrrolidine ring is optically active and possesses methyloxime functional group. Two of them have excellent in vitro antibacterial activities and pharmacokinetic profiles.

Subacute toxicity and toxicokinetics of a new antibiotic, DW-224a, after single and 4-week repeated oral administration in dogs.

The subacute toxicity and toxicokinetics of a new fluoroquinolone antibiotic, DW-224a, were evaluated after single (on the 1st day) and 4-week (on the 28th day) oral administration of the drug at doses of 0 (to serve as a control), 10, 30, and 90 mg/kg/d, to male and female dogs (n=3 for male and female dogs for each dose). During the test period, clinical signs, mortality, body weight, food consumption, ophthalmoscopy, urinalysis, hematology, serum biochemistry, gross findings, organ weight and histopathology were examined. The 4-week repeated oral dose of DW-224a resulted in vomiting, salivation, increased serum cholesterol level, and atrophy of thymus and testes.