Various antibacterial fluoroquinolone compounds were prepared by the direct amination of 7-halo-6- fluoroquinolone-3-carboxylic acids with a variety of piperazine derivatives and (4aR,7aR)-octahydro-1H-pyrrolo[3,4-b] pyridine using Zirconia Sulfuric Acid (ZrSA) nanoparticle, as a catalyst in the presence of ordinary or magnetized water upon reflux condition. The results showed that ZrSA exh...

Various antibacterial fluoroquinolone compounds were prepared by the direct amination of 7-halo-6- fluoroquinolone-3-carboxylic acids with variety of piperazine derivatives and (4aR,7aR)-octahydro-1H-pyrrolo[3,4-b] pyridine using Zirconia Sulfuric Acid (ZrSA) nanoparticle, as a catalyst in refluxing water. The results showed that ZrSA exhibited high catalytic activity towards the synthesis of f...

Food poisoning has been emerged as a worldwide health issue and related illness in both developed and developing countries confirms its significance as an important public health priority.In vitro antibacterialevaluationof nine fluoroquinolone derivatives against food borne bacteria including Gram-positive (Staphylococcus aureus) and Gram-negative (Salmonella enterica, Escherichia coli, Yersini...

a series of fluoroquinolone derivatives holding triazolidindione moieties have been synthesized and proved to be cytotoxic agents in vitro particularly against cancer cell lines (sknmc, mcf7, a2780-cp, sw48, a549, kb, ht-29, hepg 2 ). the cytotoxic activity was assessed using mtt colorimetric assay. our compounds had less cytotoxicity than doxorubicin in all studied cell lines.

Fluoroquinolones have attracted much attention because of their broad spectrum of activity against various bacteria, mycobacteria and parasites but there are numerous factors including solubility, side effects and cost of using these drugs. Drug discovery and development is a broad field that encompasses many disciplines like formation of a new moiety, methodology, potency, technology and green...

Fluoroquinolone resistance in Staphylococcus aureus results from amino acid substitutions at particular locations in the DNA gyrase A and B subunits as well as in the topoisomerase IV A subunit and from NorA-mediated efflux. More than one resistance mechanism may be present in a single strain. Fluoroquinolone-resistant derivatives of SA-1199, a methicillin-susceptible S. aureus strain, were sel...

We report in this work the antibacterial evaluation of 12 lipophilic fluoroquinolone derivatives containing diaminoalkyl side chains at C-7 position. The compounds were investigated against 15 bacterial strains including gram-negative and gram-positive species of clinical and microbiological importance. Three compounds (5, 10 and 11) were as active as or more efficient than gatifloxacin against...

In Enterobacteriaceae, the permeability of the outer membrane to hydrophilic antibiotics is associated with the presence of pore-forming proteins. We tested the diffusion of the fluoroquinolone norfloxacin in four Enterobacter cloacae strains: a clinical isolate and three derivatives variously producing or lacking the D and F porins. We analysed the entry of norfloxacin into E. cloacae cells in...

We report herein the synthesis and biological testing of several glycosylated derivatives of some fluoroquinolone antibiotics. In particular, we have prepared several glycosylated derivatives of ciprofloxacin (2) in which the carbohydrate units are linked to the free secondary amine of the piperazine unit by: (a) no linker (e.g., a glycosylamine), (b) a beta-oxyethyl linker, and (c) a gamma-oxy...