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The quinolones, especially the new quinolones (the 6-fluoroquinolones), are the synthetic antibacterial agents to rival the Beta-lactam and the macrolide antibacterials for impact in clinical usage in the antibacterial therapeutic field. They have a broad antibacterial spectrum of activity against Gram-positive, Gram-negative and mycobacterial pathogens as well as anaerobes. Further, they show good-to-moderate oral absorption and tissue penetration with favorable pharmacokinetics in humans resulting in high clinical efficacy in the treatment of many kinds of infections. They also exhibit excellent safety profiles as well as those of oral Beta-lactam antibiotics. The bacterial effects of quinolones inhibit the function of bacterial DNA gyrase and topoisomerase IV. The history of the development of the quinolones originated from nalidixic acid (NA), developed in 1962. In addition, the breakthrough in the drug design for the scaffold and the basic side chains have allowed improvements to be made to the first new quinolone, norfloxacin (NFLX), patented in 1978. Although currently more than 10,000 compounds have been already synthesized in the world, only two percent of them were developed and tested in clinical studies. Furthermore, out of all these compounds, only twenty have been successfully launched into the market. In this paper, the history of the development and changes of the quinolones are described from the first quinolone, NA, via, the first new quinolone (6-fluorinated quinolone) NFLX, to the latest extended-spectrum quinolone antibacterial agents against multi-drug resistant bacterial infections. NA has only modest activity against Gram-negative bacteria and low oral absorption, therefore a suitable candidate for treatment of systemic infections (UTIs) is required. Since the original discovery of NA, a series of quinolones, which are referred to as the old quinolones, have been developed leading to the first new quinolone, NFLX, with moderate improvements in over all properties starting in 1962 through and continuing throughout the 1970's. Especially, the drug design for pipemidic acid (PPA) indicated one of the important breakthroughs that lead to NFLX. The introduction of a piperazinyl group, which ia a basic moiety at the C7-position of the quinolone nuclei, improved activity against Gram-negative organisms broadening the spectrum to include Pseudomonas aeruginosa. PPA also showed soem activity against Gram-positive bac teria. The basic piperazine ring, which can form the zwitterionic natrure with the carboxylic acid at the C3-position, has subsequently been shown to increase the ability of the drugs to penetrate the bacterial cells resulting in enhanced activity. Further, the zwitterionic forms resulted in significant tissue penetration in the pharmacokinetics. On the other hand, the first compound with a fluorine atom at the C6-position of the related quinolone scaffold was flumequine and the compound indicated that activity against Gram-positive bacteria could be improved in the old quinolones. The addition of a flourine atom at the C6-position is essential for the inhibition of target enzymes. The results show the poten antibacterial activity and the penetration of the quinolone molecule into the bacterial cells and human tissue. The real breakthrough came with the combination of these two features in NFLX, a 6-fluorinated quinolone having a piperazinyl group at the C7-position, NFLX features significant differences from the old quinolones in the activities and pharmacokinetics in humans, resulting in high clinical efficacy in the treatment of many kinds of infections including RTIs.Consequently, those great discoveries are rapidly superseded by even better compounds and NFLX proved to be just the beginning of a highly successful period of research into the modifications of the new quinolone antibacterials. Simce the chemical structure and important features of NFLX had become apparent in 1978, many compounds were patented in the next three years, several of which reached the market. Among the drugs, ofloxacin (OFLX) and ciprofloxacin (CPFX) are recognized as superior in several respects to the oral beta-lactam antibiotics as an antibacterial agent. With a focus on OFLX and CPFX, numerous research groups entered the antibacterial therapeutic field, triggering intense competition in the search to find newer, more effective quinolones. After NFLX was introduced in the market, while resulting by the end of today, eleven kinds of other new quinolones launched in Japan. They are enoxacin (ENX), OFLX, CPFX, lomefloxacin (LFLX), fleroxacin (FRLX), tosufloxacin (TFLX), levofloxacin (LVFX), sparfloxacin (SPFX), gatifloxacin (GFLX), prulifloxacin (PULX) and also pazufloxacin (PZFX). The advantages of these compounds, e.g., LVFX, SPFX and GFLX, are that their spectrum includes Gram-positive bacteria species as well as Gram-negative bacteria and they improve bioavailability results when a daily dose is administered for systemic infections including RTIs. However, unexpected adverse reactions, such as the CNS reaction, the drug-drug interaction, phototoxicity, hepatotoxicity and cardiotoxicity such as the QTc interval prolongation of ECG, have been reported in the clinical evaluations or the post-marketing surveillance of several new quinolones. Moreover, the adverse reactions of arthropathy (the joint toxicity) predicated from studies in juvenile animals have never materialized in clinical use. Therefore, no drugs other than NFLX have yet been approved for pediatric use. Fortunately, the newer quinolones are being developed and tested to reduce these adverse reactions on the basis of recent studies. On the other hand, multi-drug resistant Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant coagulase-negative staphycolocci (MRCNS), penicillin-resistant Streptococcus pneumoniae (PRSP) and vancomycin-resistant enterococci (VRE) have been a serious problem in the medical community. Recently, the new quinolone antibacterials are highly successful class of antibacterial therapeutic field, however, the increased isolation of quinolone-resistant bacteria above them has become a normal outcome. These problems of multi-drug resistance have been the driving force for the development of newer quinolones. The next gereration of quinolone antibacterial agents will be potent against multi-drug resistant bacteria, such as MRSA, and provide a lower rate of emergence in resistance. Further, they should have favorable safety profiles to reduce the adverse reactions. The future of quinolones as the ultimate in pharmaceuticals must be handled cautiously if they are to realize their potential in the medical community.
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Resistance of Neisseria gonorrhoeae to antimicrobial agents continues to spread and intensify. Choosing an antimicrobial regimen requires knowledge of the comparative efficacy of candidate regimens, as delineated in properly conducted clinical trials; their activity against N. gonorrhoeae in vitro; and their pharmacokinetics and toxicity. We tabulated the results of trials of single-dose antimicrobial therapy for uncomplicated gonococcal infection published after 1980. Thirty regimens comprising 21 antimicrobial drugs have been shown to be highly effective for rectal and urogenital infections; the agents involved are cefixime, cefodizime, cefotaxime, cefoxitin, ceftizoxime, ceftriaxone, cefuroxime, cefuroxime axetil, ciprofloxacin, fleroxacin, norfloxacin, ofloxacin, pefloxacin, temafloxacin, azithromycin, aztreonam, netilmicin, rifampin plus erythromycin stearate, sisomicin, and spectinomycin. Few regimens have been shown to be highly effective against pharyngeal infections. Among those antimicrobial agents available for the treatment of uncomplicated gonococcal infections in the United States, ceftriaxone (125 mg), cefixime (400 mg), ciprofloxacin (500 mg), and ofloxacin (400 mg) appear to offer the best balance of proven efficacy and safety.
Genome analysis and searches of homology between the identified transporters and proteins characterized in other organisms revealed 16 open reading frames encoding putative drug efflux pumps belonging to MFS. In the case of two of them, we also have demonstrated that they function as drug efflux proteins.
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The in vitro activity of norfloxacin (MK-0366), a new oral antimicrobial agent, was compared to that of ampicillin, tetracycline, cefazolin, nitrofurantoin, nalidixic acid, and trimethoprim against 199 gram-negative urinary isolates. Among these isolates were ampicillin-resistant Escherichia coli and gentamicin-resistant Pseudomonas aeruginosa and Serratia marcescens. Norfloxacin was the most active antimicrobial agent tested against all isolates studied; it was the only agent active against P. aeruginosa and S. marcescens.
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1. In the present study, we have examined the effects of the quinolones norfloxacin (NFLX), enoxacin (ENX), ofloxacin (OFLX), tosufloxacin (TFLX), lomefloxacin (LFLX), sparfloxacin (SPFX) and grepafloxacin (GPFX) on the efflux of doxorubicin from mouse leukaemia P388/ADR cells expressing P-glycoprotein. The relationship between their partition coefficients (hydrophobicity) and effluxing potencies was also elucidated. 2. Both TFLX and SPFX strongly increased the intracellular accumulation of doxorubicin (5 micromol/L) in P388/ADR cells, but had no effect on P388/S cells not expressing P-glycoprotein. The rank of order of the potency of the quinolones (TFLX > SPFX > GPFX > NFLX) was not related directly to their hydrophobicity. These results suggest that some quinolones can reverse anticancer drug resistance. 3. Because GPFX is more highly excreted into the bile than other known quinolones, the effects of doxorubicin (10 mg/kg) or the well-known inhibitors of P-glycoprotein, namely cyclosporine A (10 mg/kg) and erythromycin (100 mg/kg), on the biliary excretion of GPFX at steady state was studied in rats. 4. Doxorubicin, cyclosporine A and erythromycin significantly decreased the biliary clearance of GPFX. Cyclosporine A and erythromycin had a much stronger inhibitory effect on the biliary excretion of GPFX than doxorubicin. These results suggest the possibility that GPFX is, at least in part, excreted into the bile by a P-glycoprotein-mediated transport mechanism.
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DTBN from N. japonicum showed anti-MRSA and anti-VRE activities. DTBN might be involved in the inhibition of DNA topoisomerase IV.
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Five new carboxymethyl flavonoids named 5-carboxymethyl-3', 4', 7-trihydroxyflavone (1), (2S)- 5-carboxymethyl-3', 4', 7-trihydroxyflavonone (2a), (2R)-5-carboxymethyl-3', 4', 7-trihydroxyflavonone (2b), (2S)-5-carboxymethyl-4', 7-dihydroxyflavonone (3), 5- carbomethoxymethyl-4', 7-dihydroxyflavone (4), and a new chromone named 5-carboxymethyl-7-hydroxychromone (5), together with two known compounds 5-carboxymethyl-4'-hydroxyflavone-7-O-β-d-glucopyranoside (6), 5-carboxymethyl-4', 7-dihydroxyflavone (7) were isolated from Selaginella moellendorffii Hieron. Their structures including absolute configuration were elucidated by extensive spectroscopic methods and experimental electronic circular dichroism (ECD) spectra. What's worth mentioning is that a carboxymethyl substituent appeared at the C-5 position of all isolated compounds, only recently discovered in genus Selaginella. Compounds 2a and 2b were identified as a pair of chiral isomers; compound 5 was discovered as the first chromone comprising a carboxymethyl side chain. Furthermore, all compounds were evaluated for their antibacterial activities against various Gram-positives and Gram-negatives, and compared to the reference drugs amoxicillin and norfloxacin. As a result, compounds 3 and 4 exhibited as potent antimicrobial agents with a broad spectrum, and compound 5 appeared as the most promising one to combat Gram-positives.
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se identificaron 174 pacientes con infección, 31.4 % con malformación del tracto urinario y 56 % con alteraciones funcionales; 76.4 % recibía profilaxis antimicrobiana. Escherichia coli fue el agente más frecuente (67 %), seguido de Klebsiella spp. (9 %) y Pseudomonas spp. (7 %). Se observó resistencia de Escherichia coli a cefalotina (58.7 %), norfloxacina (51 %), nitrofurantoína (15.5 %), cefuroxima (12.5 %), cefotaxima (15.5 %) y cefepime (5 %).
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Zielsetzung: Bakterien sind ubiquitär in der Umwelt verbreitet. Verbunden mit der wachsenden Bevölkerung, der Urbanisation und dem Zeitmangel wächst die Inanspruchnahme von Geldautomaten (ATM). Daher sollten die bakterielle Kontamination und deren Antibiotikaresistenz auf Tastaturen von ATM in der Provinz Hamadan, Iran, untersucht werden.Methode: Von 360 ATM wurden 96 randomisiert ausgewählt. Die Antibiotikaempfindlichkeit wurde im Agardiffusionstest unter Verwendung von Plättchen mit Gentamicin (10 µg), Vancomycin (30 µg), Trimethoprim/Sulfamethoxazol (25 µg), Amikacin (30 µg), Tobramycin (10 µg), Cephalotin (30 µg), Norfloxacin (5 µg) und Ceftizoxim (30 µg) ermittelt.Ergebnisse: Die höchste Kontamination wurde bei 18 (27,7%) bzw. 12 (18,5%) der ATMs von Melli und Saderat Banken nachgewiesen. Am häufigsten wurden Staphylococcus epidermidis und Pseudomonasaeruginosa je 12-mal (18,5%), Bacillus subtilis 11-mal (16,9%), Klebsiella spp. 8-mal (12.3%), Escherichia coli und Bacillus cereus je 6-mal (9,2%), Micrococcaceae spp. 5-mal (7,69%), Staphylococcus aureus 3-mal (4,6%) und Enterobacter spp. 2-mal (3,1%) nachgewiesen. Alle isolierten Bakterien waren empfindlich gegen Gentamicin, Cephalotin, Tobramycin, Amikacin, Norfloxacin und Vancomycin. Der Anteil von S. aureus mit Resistenz gegen Trimethoprim/Sulfamethoxazol betrug 50%. Schlussfolgerung: Alle untersuchten ATM Tastaturen waren mit mindestens einer Bakterienspecies kontaminiert. Daher erscheint es sinnvoll, z.B. nach dem Betreten der Wohnung, des Arbeitsbereichs oder eines Krankenhauses eine Händedesinfektion durchzuführen, um keine kritischen Pathogene in das persönliche Umfeld bzw. in das Krankenhaus einzubringen.