Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: KEGG:D00453 (OFLX)
 61 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-1,4-dihydro-4- oxoquinoline-3-carboxylic acids bearing various substituents (H, F, C1, Me, OH, OMe, OEt, OCH2F, OCHF2, OCF3, SMe) at the C-8 position was prepared and evaluated for in vitro antibacterial activity against both standard laboratory strains and bacteria resistant to quinolones such as ciprofloxacin (CPFX, 1) and ofloxacin (OFLX, 2) from clinical isolates. The 8-methyl (8a), 8-fluoro (9a), 8-chloro (10a) and 8-methoxy (12a) compounds were 4 times more potent than CPFX (1) against both gram-positive and gram-negative bacteria. But these four compounds caused injury to the chromosomes of mammalian cells at a concentration of 100 micrograms/ml. Next, a series of quinolones having various substituents (H, C1, Me, NH2, NHMe, NMe2) at the C-5 position was prepared and evaluated for antibacterial activity and injurious effect on the chromosome. We found that the 5-amino-8-methyl compound (8d) showed strong antibacterial activity (in vitro antibacterial activity of 8d is 4 times more potent than that of CPFX (1) against both gram-positive and gram-negative bacteria), reduced injury to the chromosome, and reduced quinolone-type toxicity (free from both phototoxicity at a dosage of 30 mg/kg in guinea pigs (i.v.) and convulsion-inducing activity when coadministered with fenbufen at dosage of 100 mg/kg in mice (i.p.)).
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PMID:Studies on quinolone antibacterials. IV. Structure-activity relationships of antibacterial activity and side effects for 5- or 8-substituted and 5,8-disubstituted-7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-1, 4-dihydro-4-oxoquinoline-3-carboxylic acids. 868 18

The method of CTMAB-Al(3+)-OFLX ternary complex fluorescence microscopic imaging technique was established for the determination of ofloxacin based on the capillary effect of solvent on solid supports, and the concentration in the serum after the chicken was burdened with ofloxacin tablet, the concentration in the human urines and the percentage composition in the honeies, ofloxacin tablets and eye-drops were measured with satisfaction, respectively. In the presence of pH 9. 50 NH3-NH4Cl buffer solution and PVA-124, CTMAB-Al(3+)-OFLX ternary complex can form a self-ordered ring on the hydrophobic supports with the diameter of 1.63 mm and its ring belt width of 50 microm. When a 0.20 microL droplet was spotted, the fluorescence intensity of the ring had a favorable linear relation (r = 0.999 2) with the drug concentration in the range of 3.30 x 10(-13) - 1.65 x 10(-12) mol x ring(-1) (0.60-2.98 mg x L(-1)) and the limit of detection can reach 4.10 x 10(-15) mol x ring(-1) (7.41 microg x L(-1)) with three times of signal to noise ratio. This method has been applied to the average concentration of ofloxacin in the chicken serum with the recovery of 96.4%-101.2% after two hours of being burdened with ofloxacin tablet. Then the technique was applied to the determination of ofloxacin in the three healthy volunteer's urines after oral administration with recovery of 98.2% - 106.%. It was found that the concentrations of ofloxacin in urines were the highest after three hours of taking medicine; the result was similar to reports in the literature. The residues of ofloxacin in three different honey samples were satisfactorily determined with the recoveries of 98.2% - 106.1%, and RSD was less than 2.3%. The contents of active constituent in tablet samples and eye-drops sample were determined with recoveries of 93.5%-101.5% and 95.8%-104.2%, and RSD was 3.5% and 3.6%, respectively, which were similar to marked values.
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PMID:[Determination of the ofloxacin in the biologic samples by fluorescence microscopic imaging technique]. 2224