Design, Synthesis, Molecular Docking and Antibacterial Screening of Some Quinolone Compounds

Drugs belonging to the quinolone compounds are characterized by a quicker biological activity and a broad antibacterial spectrum [1–4]. [...]

Validation and Application of an HPLC-DAD Method for Routine Therapeutic Drug Monitoring of Ceftobiprole

ABSTRACT Ceftobiprole is a fifth-generation cephalosporin approved for the treatment of pneumonia, with a broad antibacterial spectrum, including potent activity against methicillin-resistant Staphylococcus aureus. As for the other cephalosporins, high pharmacokinetic variability and concentration-dependent neurotoxicity are expected. We describe here the first simple and rapid analytical method intended for ceftobiprole serum concentration monitoring. We report the data of 5 patients treated with ceftobiprole, among who 2 developed reversible neurological disorders with high ceftobiprole serum concentration.

Antimalarial Activity of Tigecycline, a Novel Glycylcycline Antibiotic

ABSTRACT Tigecycline is a novel glycylcycline antibiotic with a broad antibacterial spectrum. Tigecycline was tested with 66 clinical isolates of Plasmodium falciparum from Bangladesh using the histidine-rich protein 2 in vitro drug susceptibility assay. The 50% and 90% inhibitory concentrations of tigecycline were 699 (95% confidence interval, 496 to 986) and 5,905 nM (4,344 to 8,028). Tigecycline shows no activity correlation with traditional antimalarials and has substantial antimalarial activity on its own.

Antibacterial Spectrum of a Novel Des-Fluoro(6) Quinolone, BMS-284756

ABSTRACT The in vitro spectrum of a novel des-fluoro(6) quinolone, BMS-284756, was compared with those of five fluoroquinolones (trovafloxacin, moxifloxacin, levofloxacin, ofloxacin, and ciprofloxacin). BMS-284756 was among the most active and often was the most active quinolone against staphylococci (including methicillin-resistant strains), streptococci, pneumococci (including ciprofloxacin-nonsusceptible and penicillin-resistant strains), andEnterococcus faecalis. BMS-284756 inhibited ≈60 to ≈70% of the Enterococcus faecium (including vancomycin-resistant) strains and 90 to 100% of theEnterobacteriaceae strains and gastroenteric bacillary pathogens at the anticipated MIC susceptible breakpoint (≤4 μg/ml). Against the nonfermenters, BMS-284756 inhibited 90 to 100% ofPseudomonas fluorescens, Pseudomonas stutzeri,Stenotrophomonas maltophilia, Flavobacteriumspp., and Acinetobacter spp. and 72% ofPseudomonas aeruginosa strains at 4 μg/ml. Against anaerobic bacteria, BMS-284756 was among the most active, inhibiting essentially all strains tested. It had very low MICs against the fastidious and atypical microbial species, in particular against mycoplasmas or ureaplasmas, Borrelia burgdorferi, chlamydia, and gonococci. These results indicate that with its broad antibacterial spectrum, BMS-284756 should be evaluated clinically for the treatment of community and nosocomial infections.