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Synthesis of gatifloxacin - Teva Pharmaceuticals USA, Inc.

Synthesis, characterization, antibacterial, antifungal and immunomodulating activities of gatifloxacin–metal complexes

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Synthesis research of gatifloxacin hydrochloride


In genetic toxicity tests, gatifloxacin was positive in 1 of 5 strains used in bacterial reverse mutation assays: Salmonella strain TA102. Gatifloxacin was positive in mammalian cell mutation and chromosome aberration assays. Gatifloxacin was positive in unscheduled DNA synthesis in rat hepatocytes but not human leukocytes. Gatifloxacin was negative in micronucleus tests in mice, cytogenetics test in rats, and DNA repair test in rats. The genotoxic findings are similar to findings obtained with other quinolones and may be due to the pharmacologic inhibitory effects of high concentrations of gatifloxacin on eukaryotic type II DNA topoisomerase.

Synthesis research of gatifloxacin hydrochloride[J]


In genetic toxicity tests, gatifloxacin was positive in 1 of 5 strains used in bacterial reverse mutation assays: Salmonella strain TA102. Gatifloxacin was positive in mammalian cell mutation and chromosome aberration assays. Gatifloxacin was positive in unscheduled DNA synthesis in rat hepatocytes but not human leukocytes. Gatifloxacin was negative in micronucleus tests in mice, cytogenetics test in rats, and DNA repair test in rats. The genotoxic findings are similar to findings obtained with other quinolones and may be due to the pharmacologic inhibitory effects of high concentrations of gatifloxacin on eukaryotic type II DNA topoisomerase.

29/03/2007 · Title: Novel synthesis of gatifloxacin

For better understanding of these interactions, complexes ofgatifloxacin were synthesized with Mg(II), Ca(II), Cr(III), Mn(II),Fe(III), Co(II), Ni(II), Cu(II), Zn(II) and Cd(II) (usually present inhuman body) and their structures were established with the help ofspectroscopic studies like IR, UV, and NMR.

Fluoroquinolone (FQ) has a broad spectrum of activity against several bacteria, mycobacteria, parasites, and other diseases. Moxifloxacin and gatifloxacin are a new generation of fluoroquinolone agents with improved activity against Gram-negative and positive bacteria. As lipophilicity is an important consideration in the design and activity of novel antibacterial agents, we report in this work the synthesis and biological evaluation of 12 lipophilic moxifloxacin or gatifloxacin derivatives, by reaction of 1-cyclopropyl-6,7-difluoro-1,4-dihydro-8-methoxy-4-oxoquinoline-3-carboxylic acid 13 with severals N-monoalkyl 1,2-ethanediamine or 1,3-propanediamine.

PDF Downloads : Oriental Journal of Chemistry

Dimethylamino-propyl, carboxy-propyl, and amino-propyl(2-methyl) derivatives of gatifloxacin (GFX), DMAP-GFX, CP-GFX, and APM-GFX, were designed and synthesized to target OCT, MCT, and ATB (0, +) transporters, respectively.

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    Synthesis, characterization, antibacterial, antifungal and immunomodulating activities of gatifloxacin-metal complexes

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