人工合成抗菌药ppt.pptxVIP

 Synthetic antimicrobial agents(人工合成抗菌药);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. ;Chemistry Derived from basic structure of nalidixic acid (萘啶酸)and have substituents at N-1, C-5, C-7, position 8 and a fluorine atom at position 6. Fluorine at position 6 enhances gyrase inhibition and cell penetration. ;Chemical structure;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;Summary of antimicrobial spectrum of quinolones. ;Typical therapeutic applications of uoroquinolones.;First-generation agents(1962-1969) Nalidixic acid, 萘啶酸 The first generation drug of the quinolone antibiotics Moderate gram-negative activity and minimal systemic distribution Clinical applications Uncomplicated urinary tract infections ;Second-generation quinolones (1969-1979) Pipemidic acid 吡哌酸 Cinoxacin西诺沙星 Expanded gram-negative activity and atypical pathogen coverage, but limited gram-positive activity. Most active against aerobic gram-negative bacilli Ciprofloxacin remains the quinolone most active against Pseudomonas aeruginosa ;Second-generation quinolones (1969-1979) Active against gram-positive and gram-negative bacteria, mycobacteria, mycoplasma支原体and legionella species军团杆菌属.? Longer half-lives due to slow elimination, distribution into many tissues and body fluids and penetration into human c