Levofloxacin左氧氟沙星Ciprofloxacin环丙沙星Ofloxacin氧氟沙星.PPTVIP

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Levofloxacin左氧氟沙星Ciprofloxacin环丙沙星Ofloxacin氧氟沙星.PPT

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Levofloxacin左氧氟沙星Ciprofloxacin环丙沙星Ofloxacin氧氟沙星

Part6 Synthetic antimicrobial agents(人工合成抗菌药) Huifang Tang tanghuifang@zju.edu.cn Classification of Synthetic antimicrobial agents General features Broad antimicrobial activity and are effective after oral administration for the treatment of a wide variety of infectious disease. Relatively few side effects. Microbial resistance to their action does not develop rapidly. Classification Generation Examples 1 st (1962-1969) Nalidixic acid, 萘啶酸 2 nd (1969-1979) Pipemidic acid 吡哌酸 Cinoxacin 西诺沙星 3 rd (1980-1996) Norfloxacin 诺氟沙星 Levofloxacin 左氧氟沙星 Ciprofloxacin 环丙沙星 Ofloxacin 氧氟沙星 sparfloxacin 司帕沙星 4 th (1997-) Grepafloxacin 格帕沙星 Clinafloxacin 克林沙星 Gatifloxacin 加替沙星 Moxifloxacin 莫西沙星 Antimicrobial activity spectrum (1) Bactericidal and have significant PAE. (2)Excellent activity against aerobic gram-negative bacteria, some agents have activity against Pesudomonas. (3) Several newer agents with improved activity against aerobic gram-positive bacteria. Antimicrobial activity spectrum (4) They also are effective against Chlamydia spp.（衣原体）, Legionella pneumophila(军团菌) ,anaerobic bacteria, mycobacteria(分枝杆菌). (5) Some agents have limited activity against multiple-resistance strains. （6）Bactericidal concentration≥ bacteriostatic concentration The function of DNA gyrase is to introduce supercoils into the linear DNA double helix, which results in the highly condensed 3-dimensional structure of the DNA usually present inside the cell. DNA gyrase consists of two proteins (A and B), with the active species being a heterotetramer (A2B2). (1) Mutation of the gyrA gene that encoded the A subunit polypeptide can confer resistance to these drugs. (2) Mutation of the gene cfxB and nfxB that encoded the porin decreased permeability of cell membrance. (3) The high expression