Mechanism of action of fluoroquinolones: the basics...
2 key enzymes in DNA replication:
Ternary complex DNA - enzyme - fluoroquinolone
Resistance to fluoroquinolones: the basics
Fluoroquinolones are the first entirely man-made
antibiotics: do we understand our molecule ?
Chemistry and Activity
The pharmacophore common to all fluoroquinolones
From chloroquine to nalidixic acid...
From nalidixic acid to 1st generation
"1st generation" fluoroquinolones
The "first generation" of fluoroquinolones
From ofloxacin to levofloxacin...
The "first generation" of fluoroquinolones and
From first to second generation of fluoroquinolones
From second to third generation of fluoroquinolones
Maintenance of anti - Gram (-) activity
Gram (-) activity (E. coli)
Improving Gram (+) activity (S. pneumoniae)
Activity against S. pneumoniae
Activity against anaerobes ...
Activity against B. fragilis
Is there a SAR for emergence of resistance ?
Fluoroquinolones with a C8-methoxy
Frequent side effects of fluoroquinolones: is there
a SAR ?
SAR of frequent side effects
Fluoroquinolones with low or no drug interactions..
Fluoroquinolones with high phototoxicity ...
Rare side effects of fluoroquinolones:
Rare side effects of fluoroquinolones: cardiac
Cardiac toxicity QT prolongation: is there any
Other severe toxicities
Which part of the molecule is the culprit ?
SAR of pharmacokinetic parameters
SAR of main pharmacokinetic parameters: how to
get a long half life
SAR of main pharmacokinetic parameters: biodisponibility
SAR of main pharmacokinetic parameters: volume
Resistance: do not forget the correct dosing...
Pharmacokinetic parameters in relation with efficacy
Indications of new fluoroquinolones
Shall we have a very bright future ?
Home Page: http://www.md.ucl.ac.be/facm