First generation fluoroquinolones norfloxacin ciprofloxacin piperazine cyclo propyl x methyl H3c pefloxacin ofloxacin morpholine
First generation fluoroquinolones
From ofloxacin to levofloxacin Ofloxacin is a racemic mixture H Levofloxacin is the pure(-)S isomer The active form of ofloxacin is the(-)S isomer Eur. pat. 206, 283 to Daiichi, 1987
From ofloxacin to levofloxacin
Fluoroquinolones c H CO sparfloxacin moxifloxacin 0.125-0.5 0.01-0.5 ciprofloxacin 05-2 temafloxacin trovafloxacin 05-1 0.007-0.25
Fluoroquinolones
Fluoroquinolones broad antimicrobial activity effective after oral administration relatively few side effects resistance to their action does not develop rapidly
• broad antimicrobial activity • effective after oral administration • relatively few side effects • resistance to their action does not develop rapidly. Fluoroquinolones
General properties of Quinolones 1. Antimicrobial activity spectrum (1) bactericidal and have significant PAE. (2 aerobic G- bacteria, Pesudomonas aerobic Gt bacteria, Chlamydia spp.(A 原体), Legionella pneumophila(军团菌) anaerobic bacteria, mycobacteria(分枝杆 #), multiple-resistance strains
1. Antimicrobial activity & spectrum: (1) bactericidal and have significant PAE. (2) aerobic G- bacteria, Pesudomonas, aerobic G+ bacteria, Chlamydia spp.（衣 原体）, Legionella pneumophila(军团菌) , anaerobic bacteria, mycobacteria(分枝杆 菌), multiple-resistance strains. General properties of Quinolones