A series of novel 7-(3-amino-6,7-dihydro-2-methyl-2H-pyrazolo[4,3-c]pyridin- 5(4H)-yl)fluoroquinolone derivatives were designed, synthesized and characterized by 1H-NMR, MS and HRMS. These fluoroquinolones were evaluated for their in vitro antibacterial activity against representative Gram-positive and Gram-negative strains. Results reveal that most of the target compounds exhibit good growth i...

The respiratory fluoroquinolones moxifloxacin, gemifloxacin, and high-dose levofloxacin are recommended in guidelines for effective empirical antimicrobial therapy of community-acquired pneumonia (CAP). The use of these antibiotics for this indication in areas with a high prevalence of tuberculosis (TB) has been questioned due to the perception that they contribute both to delays in the diagnos...

Streptococcus pneumoniae is an important pathogen in many community-acquired respiratory infections in the United States and a leading cause of morbidity and mortality worldwide. Unfortunately, S. pneumoniae is becoming increasingly resistant to a variety of antibiotics. Results of recent surveillance studies in the United States show that the prevalence of penicillin-nonsusceptible S. pneumoni...

T-3811, the free base of T-3811ME (BMS-284756), a new des-F(6)-quinolone, showed a potent in vitro activity (MIC at which 90% of the isolates tested are inhibited [MIC(90)], 0.0313 microg/ml) against Mycoplasma pneumoniae. The MIC(90) of T-3811 was 4-fold higher than that of clarithromycin but was 4- to 8-fold lower than those of trovafloxacin, gatifloxacin, gemifloxacin, and moxifloxacin and w...

Despite an increasing population of patients with chronic renal insufficiency, the literature on the management of urinary tract infections (UTI) in these patients is sparse. Patients with underlying diabetes are a specific population at risk. Antimicrobial treatment of UTI requires adequate serum, renal, parenchymal, and urine concentrations of drugs with antibacterial activity versus the etio...

Nuclear medicine imaging has been used to localize infection sites and efforts have been continued to develop modified infection specific radiopharmaceuticals. In this study gemifloxacin as a broad-spectrum quinolone has been labeled with [99mTc (CO)3 (H2O)3]+ core in order to evaluate its feasibility as an infection imaging agent for in vivo use. The stability of radioconjugate was checked in ...