Clinafloxacin - CAS 105956-97-6
Catalog number: B0084-053762
Category: Inhibitor
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Clinafloxacin is a fluoroquinolone antibiotic with a broad-range of antibacterial activity. It inhibits both DNA gyrase and topoisomerase IV.
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B0084-053762 100 mg $198 In stock
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Pale Beige Solid
7-(3-aminopyrrolidin-1-yl)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
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1.Synthesis of (99m)TcN-clinafloxacin Dithiocarbamate Complex and Comparative Radiobiological Evaluation in Staphylococcus aureus Infected Mice.
Shah SQ1, Khan MR2. World J Nucl Med. 2014 Sep;13(3):154-8. doi: 10.4103/1450-1147.144813.
Clinafloxacin dithiocarbamate (CNND) preparation and radiolabeling through [(99m)Tc ≡ N](2+) core with the gamma (γ) emitter ((99m)Tc) was assessed. The potentiality of the (99m)Tc(V) ≡ N-CNND complex was investigated as perspective a Staphylococcus aureus (S.a.) in vivo infection radiotracer in terms of radiochemical stability in normal saline (n.s.), human serum (h.s.), binding efficacy with live and heat killed S.a. and biodistribution in female nude mice model (FNMD). More than 90% stability was observed in n.s. for 4 h with the highest yield of 98.70 ± 0.26% at 30 min after reconstitution. In h.s., the (99m)Tc(V) ≡ N-CNND complex was found stable up to 16 h with 15.35% side products. Maximum in vitro binding (68.75 ± 0.80%, 90 min) with S.a. was observed after 90 min of incubation. In FNMD, (infected with live strain) approximately six-fold higher uptakes was noted in the infected to inflamed and normal muscles. The higher stability in n.
2.Design and biological evaluation of novel quinolone-based metronidazole derivatives as potent Cu(2+) mediated DNA-targeting antibacterial agents.
Zhang L1, Kumar KV1, Geng RX2, Zhou CH3. Bioorg Med Chem Lett. 2015 Sep 1;25(17):3699-705. doi: 10.1016/j.bmcl.2015.06.041. Epub 2015 Jun 16.
A series of novel quinolone-based metronidazole derivatives as new type of antimicrobial agents were developed and characterized. Most of them gave good antibacterial activity towards the Gram-positive and negative bacteria. Noticeably, quinolone derivative 3i exhibited low MIC value of 0.25 μg/mL against Pseudomonas aeruginosa, which was even superior to reference drugs Norfloxacin, Ciprofloxacin and Clinafloxacin. The further research revealed that compound 3i could intercalate into P. aeruginosa DNA through copper ion bridge to form a steady 3i-Cu(2+)-DNA ternary complex which might further block DNA replication to exert the powerful bioactivities.
3.Heat stable antimicrobial activity of Burkholderia gladioli OR1 against clinical drug resistant isolates.
Bharti P1, Anand V, Chander J, Singh IP, Singh TV, Tewari R. Indian J Med Res. 2012 May;135(5):666-71.
BACKGROUND & OBJECTIVES: Drug resistant microbes are a serious challenge to human health. During the search for novel antibiotics/inhibitors from the agricultural soil, a bacterial colony was found to inhibit the growth of clinical isolates including Staphylococcus (resistant to amikacin, ciprofloxacin, clindamycin, clinafloxacin, erythromycin, gentamicin and methicillin) and Candida (resistant to fluconazole and itraconazole). The culture was identified as Burkholderia gladioli and produced at least five different antimicrobial compounds which were highly stable at high temperature (121 o C) and in the broad pH range (3.0-11.0). We report here the antimicrobial activity of B. gladioli against drug resistant bacterial pathogens.
4.Relationship of cellular topoisomerase IIα inhibition to cytotoxicity and published genotoxicity of fluoroquinolone antibiotics in V79 cells.
Williams GM1, Brunnemann KD, Smart DJ, Molina D, Jeffrey AM, Duan JD, Krebsfaenger N, Kampkoetter A, Schmuck G. Chem Biol Interact. 2013 Apr 25;203(2):386-90. doi: 10.1016/j.cbi.2013.01.003. Epub 2013 Jan 20.
Fluoroquinolone (FQ) antibiotics are bacteriocidal through inhibition of the bacterial gyrase and at sufficient concentrations in vitro, they can inhibit the homologous eukaryotic topoisomerase (TOPO) II enzyme. FQ exert a variety of genotoxic effects in mammalian systems through mechanisms not yet established, but which are postulated to involve inhibition of TOPO II enzymes. To assess the relationship of inhibition of cell nuclear TOPO II to cytotoxicity and reported genotoxicity, two FQ, clinafloxacin (CLFX) and lomefloxacin (LOFX), having available genotoxicity data showing substantial differences with CLFX being more potent than LOFX, were selected for study. The relative inhibitory activities of these FQ on nuclear TOPO IIα in cultured Chinese hamster lung fibroblasts (V79 cells) over dose ranges and at equimolar concentrations were assessed by measuring nuclear stabilized cleavage complexes of TOPO IIα-DNA. Cytotoxicity was measured by relative cell counts.
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CAS 105956-97-6 Clinafloxacin

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