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Gemifloxacin mesylate efficacy of the chemical structural features of their relationship by wqecv thbtn





Article Author Biography
Gemifloxacin mesylate efficacy of the chemical structural features of their relationship by
Article Posted: 06/19/2011
Article Views: 119
Articles Written: 1385
Word Count: 790
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Gemifloxacin mesylate efficacy of the chemical structural features of their relationship


 
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Since 1962 the United States and other Sterling-Winthrop Research Institute Lesher discovered the first quinolones nalidixic acid has anti-bacterial because of its broad spectrum antibacterial activity, and convenient administration, and no cross-resistance to commonly used drugs, the price more substantial effect

Antibiotic And low, become the world racing to develop production and application of key drugs, has developed the fourth generation. Compared with the previous three generations, and its structure was modified in antibacterial activity, antibacterial range, pharmacokinetic properties and have shown significant changes in plasma half-life. Fourth-generation fluoroquinolones both to retain the previous three generations of anti-Gram-negative bacteria activity? Has significantly enhanced the anti-Gram-positive activity, while Legionella, mycoplasma, chlamydia show a strong effect in particular, to improve the antibacterial activity of anaerobic bacteria. And efficacy of its antimicrobial activity with the third generation

Cephalosporin Streptomyces comparable to some of the antimicrobial spectrum and antimicrobial products has reached or exceeded the capacity of -acyl

Amines Antibiotics, even to the carbapenem antibiotic target.

Gemifloxacin mesylate (domestic trade name: Super Star Kyrgyzstan) Korea

LG Company and British co-developed by GSK fourth-generation fluoroquinolone antibacterial drug, in April 2003 approved by the FDA in the United States, in July 2006 approved by SFDA in China market. Gemifloxacin is a broad-spectrum fungicide fast, particularly in enhancing the role of anti-G + bacteria, pneumonia

Streptococcus Showed strong antibacterial activity and antibacterial activity against -lactam and macrolide antibiotic sensitive and resistant to impact. Methicillin-resistant Staphylococcus aureus and respiratory pathogens, such as

Influenza Haemophilus, mucositis Mora pneumococcal bacteria and have a good effect. In vitro antibacterial activity test showed that gemifloxacin activity against Streptococcus pneumoniae compared with ciprofloxacin, sparfloxacin, grepafloxacin and moxifloxacin and other stronger, as 30 to 60 times as ciprofloxacin and levofloxacin 15 ~ 30 times; resistant to penicillin and erythromycin in different strains of pneumonia and antibacterial activity of ciprofloxacin higher than the 16 to 64 times; on Haemophilus influenzae, Moraxella catarrhalis, Escherichia coli, pneumonia Klebsiella than ciprofloxacin and levofloxacin. Compared with these drugs? Its has the lowest M

IC 90 (0.03 ~ 0.06 g/ml). Legionella, mycoplasma, chlamydia and that is very active in the Pro

Bed Can be used for the treatment of respiratory tract infections. In addition, gemifloxacin has a good post-antibiotic effect (

PA E). Gemifloxacin is the seventh in the introduction of fluoroquinolones oxime - pyrrolidinyl get new drugs, the most prominent of the Department is significantly enhanced with the target site?? Affinity of topoisomerase IV compared to the third generation of quinolones such as ciprofloxacin has greatly improved its antibacterial spectrum, especially for G + bacteria were significantly more bactericidal.

Fluoroquinolone antibacterial ability is the same with DNA gyrase / topoisomerase IV and DNA binding to the complexes. Gemifloxacin molecules through the 3 - and 4-carbonyl - carboxylic hydrogen bond and the DNA and the enzyme linked to form a base on the ternary complex, continuous integration and complex stabilization, leading to cell death,

Table Now the antibacterial activity of drugs. Gemifloxacin is highly selective, sterilization is the main target topoisomerase IV.

Gemifloxacin pyrrole alkyl side chain increased the lipophilic derivatives, help to improve anti-G + bacteria and

Copper Green Pseudomonas activity. Gemifloxacin with 7 side chain has a unique A oxime (CH3O-N =) structure, structure-activity relationship shows that the impact of the special structure of its antimicrobial spectrum of prominent anti-G + bacteria can enhance the activity, if other, more methyl large groups or hydrogen to replace all its activity decreased or even disappeared. The most prominent feature is the pair of fluoroquinolone resistance in Streptococcus pneumoniae sensitive and have high activity, superior to trovafloxacin and ciprofloxacin, for on fluoroquinolone resistance or sensitive Staphylococcus aureus and GPB The antibacterial activity stronger than the latter two. Anti-G-bacteria activity and ciprofloxacin, particularly Haemophilus influenzae and Klebsiella pneumoniae with high activity. The anti-anaerobic activity and trovafloxacin is better than that of levofloxacin and so on and so atypical bacteria Mycoplasma pneumoniae also had good activity.

Gemifloxacin brought a new structure is strong efficacy and high

Security Sex. Its efficacy is not only far stronger than the third-generation quinolone, as following ofloxacin, ciprofloxacin, also better than the fourth generation with the generation of quinolones. At the same time, their safety was also higher than gatifloxacin and other. Gemifloxacin, as a new oral broad-spectrum fluoroquinolone antibiotic, on respiratory tract infection pathogens Streptococcus pneumoniae, Haemophilus influenzae, Moraxella catarrhalis and atypical pathogens have a good effect.

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