Azole antifungal ketoconazole (KET) was demonstrated to activate aryl hydrocarbon receptor (AhR). Since clinically used KET is a racemic mixture of two cis-enantiomers (2R,4S)-(+)-KET and (2S,4R)-(-)-KET, we examined the effects of KET enantiomers on AhR signaling pathway. (+)-KET dose-dependently activated AhR in human gene reporter cell line AZ-AHR, and displayed 5-20× higher agonist activity...

Eighty-nine patients with uncomplicated gonorrhea, including 31 patients (34.8%) infected with penicillinase-producing strains of Neisseria gonorrhoeae, were treated with oral ofloxacin (single 400-mg dose) or intramuscular ceftriaxone (250-mg dose). All 47 patients who received ofloxacin and 41 of 42 patients who received ceftriaxone were cured.

The in vitro susceptibilities of 12 strains of Chlamydia pneumonia to a new quinolone, OPC-17116; ofloxacin; and sparfloxacin were determined. OPC-17116 was slightly less active than sparfloxacin but more active than ofloxacin, with a MIC for 90% of strains tested and a minimal chlamydiacidal concentration for 90% of strains tested of 0.5 micrograms/ml.

The racemate and the enantiomers of cytosporone E [3-heptyl-4,5,6-trihydroxyphthalide (1)], a metabolite of the endophytic fungus, CR200 (Cytospora sp.), were synthesized. The key steps were (i) Sharpless asymmetric dihydroxylation of an alkene (8) and (ii) HPLC separation of the enantiomers of tert-butyldimethylsilyl ether (12) on a chiral stationary phase. The racemate and enantiomers of cyto...

PURPOSE To determine whether a 3-day application of ofloxacin results in the selection of fluoroquinolone-resistant conjunctival coagulase-negative Staphylococcus. DESIGN Prospective randomized trial. METHODS Patients scheduled for ocular surgery were randomized to a control (89 eyes) or study group (70 eyes). The study group received topical ofloxacin (0.3%) four times a day for 3 days. Co...

A simple, specific and stability indicating liquid chromatographic method was developed and validated for the simultaneous determination of ofloxacin and prednisolone acetate in bulk and pharmaceutical formulations. Optimum separation was achieved in less than 5 min using a C18 column (150 mmx4.6 mm i.d, 3μ particle size) by isocratic elution. The mobile phase consisting of a mixture of 0.01M p...

The influence of multiple doses of ofloxacin (ORF 18489) on the disposition of theophylline was studied in 15 male volunteers. Subjects were confined in the Clinical Research Unit for 13 days and given a xanthine-free diet. A single dose (3 mg/kg) of theophylline was given orally, and blood samples were collected at fixed time intervals for 36 h. The concentrations of theophylline were measured...

Mycoplasma hominis mutants were selected stepwise for resistance to ofloxacin and sparfloxacin, and their gyrA, gyrB, parC, and parE quinolone resistance-determining regions were characterized. For ofloxacin, four rounds of selection yielded six first-, six second-, five third-, and two fourth-step mutants. The first-step mutants harbored a single Asp426-->Asn substitution in ParE. GyrA changes...

High levels of antibiotic tolerance are a hallmark of bacterial biofilms. In contrast to well-characterized inherited antibiotic resistance, molecular mechanisms leading to reversible and transient antibiotic tolerance displayed by biofilm bacteria are still poorly understood. The physiological heterogeneity of biofilms influences the formation of transient specialized subpopulations that may b...