Pazufloxacin

Molecular formula C16H15FN2O4 Molecular weight 318.30 CAS Registry No 127045-41-4 Merck Index 13, 7128 

Sample preparation Vortex 50 xL plasma with 350 xL 1 p,g/mL IS in MeOH, centrifuge. Evaporate the supernatant to dr5mess under a stream of nitrogen at 40°, reconstitute the residue with mobile phase, inject an aliquot. 

Mobile phase MeCN l M ammonium acetate 50 mM citric acid 15 1 84 

Hasegawa, T. Nadai, M. Haghgoo, S. Yamaki, K. Takagi, K. Nabeshima, T. Influence of a newly developed quinolone, T-3761, on pharmacokinetics of theophylline in rats, Antimicrob.Agents Chemother., 1995,39, 2138-2140. 

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More then a dozen representatives of the above ring systems were introduced into the human therapy. Actisomide (2) and trequinsin (3) are used as antiarrhytmic and antihypertensive agents, respectively. Sunepitron (4), a a 2-adrenoceptor antagonist, is under clinical trials for the treatment of anxiety and depression. Representatives of the third generation of antibacterial quinolone-3-carboxylic acids the blockbluster ofloxacin (5), its levorotatory enantiomer, levofloxacin (6), and rufloxacin (7) have gained wide acceptance for the treatment of bacterial infections of the respiratory and urinary tracts, skin, and soft tissues, as well as sexually transmitted diseases, and pazufloxacin (8) is under development. Praziquantel (9) is widely applied for the treatment of schistosomes- and cestode-caused infection in both veterinary and human therapies (Scheme 4). 

Assay and analysis of pazufloxacin (8) and its related substances were established by HPLC (98MI89). 

Preparation and usage of nitrate salt of 5 and pazufloxacin (8) were patented (01MTP14). 

Graphical synthetic routes of pazufloxacin (8) was reported (99MI25). 

A chemiluminescence method was developed for determination of pazufloxacin mesylate (08MI85). Pazufloxacin was determined in formulation using water-soluble quantum dots as fluorescent probe (08MI86). A molecularly imprinted polymer was developed, and it exhibits higher affinity and selectivity for pazufloxacin than for norfloxacin and ofloxacin (05MI31). 

Fluoride in pazufloxacin mesylate samples was determined by 19F NMR spectra (06MI61,62). Platina complexes of ofloxacin and levoflox-acin were characterized by 1H, 13C, and 195Pt NMR (09ICA2060). and 13C NMR spectra of quaternary derivative 175 of ofloxacin were determined in both acidic and alkaline solutions (08MI91). Mg complexes of ofloxacin [Mg(Oflo)2(H20)2-2H20] and levofloxacin [Mg (Levo)2(H20)2 2H20] were characterized by [H and 13C NMR spectra (06JIB1755). 

Niki Y, Watanabe S, Yoshida K, Miyashita N, Nakajima M, Matsushima T. Effect of pazufloxacin mesi-late on the serum concentration of theophylline. J Infect Chemother 2002 8(l) 33-6. 

Pazufloxacin is an injectable quinolone antibiotic with bactericidal effect against cephalosporin-resistant, carbapenem-resistant, and aminoglycoside-resistant strains of bacteria. 

In in vivo studies in animal models of phototoxicity, pazufloxacin was less potent than nalidixic acid, ofloxacin, ciprofloxacin, or sparfloxacin, and there was no photoallergenicity (1). 

Co-administration of pazufloxacin and theophylline has been studied in rats (2). Pazufloxacin reduced the clearance of theophylline by about 25%. In seven healthy volunteers taking modified-release theophylline, intravenous pazufloxacin mesilate increased serum theophylline concentrations analysis of the urinary excretion of theophylline and its metabolites suggested that CYP1A2 had been inhibited (2). Theophylline concentrations need to be monitored if pazufloxacin is co-administered. 

Nagasawa M, Nakamura S, Miyazaki M, Nojima Y, Hayakawa H, Kawamura Y. [Phototoxicity studies of pazufloxacin mesilate, a novel parenteral quinolone antimicrobial agent—in vitro and in vivo studies.) Jpn J Antibiot... 

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