In vitro selection techniques offer powerful and versatile methods to isolate nucleic acid sequences with specific activities from huge libraries. We describe an in vitro selection strategy for the de novo selection of allosteric self-cleaving ribozymes responding to pefloxacin and other quinolone derivatives. Within 16 selection cycles, highly sensitive clones responding to drug levels in the ...

A simple, rapid and sensitive spectrofluorimetric method for the determination of fluoroquinolone antibiotics, norfloxacin (NOR), ciprofloxacin (CIP) and pefloxacin (PEF) is described. The method is based on the radiative energy transfer from fluoroquinolones to terbium ions (Tb3+) in the presence of tri-n-octylphosphine oxide (TOPO) in weakly acidic (pH 5.5) micellar solution of cetylpyridiniu...

UNLABELLED Recently antimicrobials of the fluoroquinolone class (pefloxacin and ofloxacin) were found far more effective against Mycobacterium leprae in studies with both mice and patients than dapsone and clofazimine. As multicentre trial participants, we evaluated the therapeutic efficacy, in terms of rate of relapse, of two new multidrug regimens containing ofloxacin, comparing them to 1 yea...

The activities of fluoroquinolones and a new macrolide against 30 clinical isolates of Mycobacterium tuberculosis were determined in vitro by agar diffusion. In order of relative potencies against M. tuberculosis, temafloxacin (MIC for 90% of isolates [MIC90], 2.3 micrograms/ml) was at least as active as the reference quinolones ofloxacin (MIC90, 2.4 micrograms/ml) and ciprofloxacin (MIC90, 4.3...

The present work describes a method based on solid-phase extraction (SPE) and ultra-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) for the simultaneous determination of three quinolones (pipemidic acid, oxolinic acid and flumequine) and twelve fluoroquinolones (marbofloxacin, fleroxacin, pefloxacin, levofloxacin, norfloxacin, ciprofloxacin, enrofloxacin, danofloxacin, l...

The behavioral and convulsant effects of cefazolin, a beta-lactam derivative, were studied after intraperitoneal administration to DBA/2 mice, a strain genetically susceptible to sound-induced seizures, and Swiss mice. DBA/2 mice were more susceptible to seizures induced by cefazolin than were Swiss mice. The proconvulsant effects of some quinolones on seizures evoked by intraperitoneal adminis...

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...

The purpose of this study is to predict human jejunal permeability (P(eff)) and fraction absorbed in human (%F(a)) for a group of antibacterial fluoroquinolones (FQs), by using a biophysical model based on measured Caco-2 permeability. The predicted P(eff) (in 10(-4) cm · s(-1) units) ranged from 0.7 (norfloxacin) to 4.5 (pefloxacin). The calculated %F(a) for norfloxacin = 51% (lit. 35%) and fo...

Because of their antimicrobial activity and pharmacologic properties, fluoroquinolones should be particularly suitable for the treatment of lower respiratory tract infections, although they might be less efficient in pneumococcal diseases. In fact, the overall clinical success rate of enoxacin, ofloxacin, pefloxacin, and ciprofloxacin is greater than 85%, and their efficacy compares favorably w...