Ninety quinolones were evaluated to determine whether their ability to induce mammalian topoisomerase II mediated DNA cleavage in vitro correlated with their antitumor activity in vivo. Ten quinolones generated linear DNA at a yield of more than 10% of substrate supercoiled DNA in the mammalian topoisomerase II mediated DNA cleavage assay. All of these compounds showed a significant increase in...

Quinolones are synthetic broad-spectrum antibiotics with good oral absorption and excellent bioavailability. Due to the chemical functions found on their nucleus (a carboxylic acid function at the 3-position, and in most cases a basic piperazinyl ring (or another N-heterocycle) at the 7-position, and a carbonyl oxygen atom at the 4-position) quinolones bind metal ions forming complexes in which...

Introduction: Fluoroquinolones are potent inhibitors of bacterial topoisomerase II. They can also inhibit eukaryotic topoisomerase, and may confer antitumoral properties. Method: In this study the antitumoral activity of a new series of N-substituted piperazinylfluoroquinolones against a panel of human tumor cell lines was determined by MTT assays. Results: Among the tested compounds N-[2- (5-b...

Abstract: A series of N-[2-(8-metoxy-2H-chromen-2-one)ethyl] piperazinyl quinolones containing a carbonyl related functional groups (oxo or oxyimino) on the ethyl spacer of coumarin and piperazin rings was synthesized and studied for their antibacterial and antifungal activities . The synthesis of compounds (6a-6l) was achieved through the versatile and efficient synthetic route that involved r...

Abstract: A series of N-[2-(8-metoxy-2H-chromen-2-one)ethyl] piperazinyl quinolones containing a carbonyl related functional groups (oxo or oxyimino) on the ethyl spacer of coumarin and piperazin rings was synthesized and studied for their antibacterial and antifungal activities . The synthesis of compounds (6a-6l) was achieved through the versatile and efficient synthetic route that involved r...

PURPOSE To assess the in vitro susceptibility of Streptococcus pneumoniae, Staphylococcus aureus and coagulase-negative staphylococci (CoNS) ocular isolates to antibiotics, and identify changing trends in resistance over a 10-year period. METHODS All isolates from ocular infections collected between 2000 and 2009 were prospectively tested against several antibiotics in vitro. S. pneumoniae is...

The cultivation of Neisseria gonorrhoeae by use of fastidious broth (FB) was evaluated. FB was found to be able to support the growth of all N. gonorrhoeae strains tested in this study without a rapid decrease in the viable count after exponential growth. After 24 h of incubation at 35 degrees C with 5% CO(2), viable counts of all strains reached over 10(8) CFU/ml in FB. Similar growth of the w...

Regioselective synthesis of quinolone-1,2,4-triazoles was established starting from 4-hydroxyquinol-2-ones. The strategy started by the reaction ethyl bromoacetate with 4-hydroxyquinoline to give corresponding oxoquinolinyl acetates, which reacted hydrazine hydrate afford hydrazide derivatives. Subsequently, hydrazides isothiocyanate derivatives acyl thiosemicarbazides. Finally, subjecting thio...

Background and Aim: Bacterial infection is common after acute variceal bleed (AVB) in patient with cirrhosis associated higher re-bleed mortality rate. Antibiotics prophylaxis ceftriaxone recommended AVB. Aim of this study was to evaluate incidence bacterial AVB during hospital stay even antibiotic prophylaxis. Methods: Retrospective analysis data patients who were on antibiotics from day 1 adm...