Novel analogues of N-piperazinyl fluoroquinolones were prepared and evaluated against a panel of Gram-positive and Gram-negative bacteria, to study the effect of introducing bulky anthracene and phenanthrene moieties on the antibacterial effects of norfloxacin, ciprofloxacin and gatifloxacin. Although most of the novel synthesized compounds had lower antibacterial effects, some derivatives show...

The in vitro activities of DC-159a against seven species of Mycobacterium were compared with moxifloxacin, gatifloxacin, levofloxacin, and rifampin. DC-159a was the most active compound against quinolone-resistant multidrug-resistant M. tuberculosis (MIC(90), 0.5 microg/ml) as well as drug-susceptible isolates (MIC(90), 0.06 microg/ml). The anti-tubercle bacilli activity of DC-159a was 4- to 32...

The electrochemical behavior of gatifloxacin (GTFX) and its interaction with natural calf thymus DNA (ctDNA) is investigated by differential pulse voltammetry (DPV) on a carbon paraffined electrode. According to the suggested electrochemical equation, a binding constant of 1.7058 x 10(5) (mol L(-1))(-1) and binding sizes s = 3.09 (base pairs) of GTFX with ctDNA are obtained by nonlinear fit ana...

We compared the in vitro antimycobacterial activity of a new fluoroquinolone, HSR-903, with strong activity against gram-positive cocci with those of levofloxacin (LVFX), sitafloxacin (STFX), and gatifloxacin (GFLX). The MICs of the quinolones for Mycobacterium tuberculosis and Mycobacterium avium complex were in the order STFX approximately GFLX < LVFX <== HSR-903 and STFX <== GFLX <== HSR-903...

We have developed a rapid new in vivo method for screening experimental drugs for their activity against Mycobacterium tuberculosis by using the gamma interferon gene-disrupted (GKO) C57BL/6 mouse. Due to the rapid growth of the infection, statistical differences indicating positive efficacy of active compounds can be seen after only 8 days of treatment. To validate this model, several fluoroqu...