چكيده لاتين :
Quinolones are a very important family ofantibacterial agents that are widely prescribed for
the treatment of infections in humans. Since their discovery in the early 1960s, the quinolone
group of antibacterials has generated considerable clinical and scientific interest. Two
major groups of compounds have been developed from the basic molecule: quinolones and
naphthyridones. The 4-pyridone-3-carboxylic acid associated with a 5, 6-fused aromatic ring
is the common chemical feature of bactericidal quinolones. In the resulting bicyclic ring, the
1-, 5-, 6-, 7-, and 8-positions are the major targets of chemical variation. Manipulations of the
basic molecule, including replacing hydrogen with fluorine at position 6, substituting a cyclic
amine residue at position 7 and adding new residues at position 1 of the quinolone ring, have
led to improved breadth and potency of antibacterial activity and pharmacokinetics. One ofthe
most significant developments has been the improved anti-Gram-positive activity of the newer
compounds, such as moxifloxacin and garenoxacin. However, some ofthese structural changes
have been found to correlate with specific adverse effects: the addition of fluorine or chlorine
at position 8 being associated with photoreactivity, e.g. sparfloxacin; and the substitution of
an amine or a methyl group at position 5 having a potential role in QTc prolongation, e.g.
sparfloxacin and grepafloxacin. The clinical utility of this expanding class of antimicrobial
agents, and the lower propensity for the development of resistance with the newer quinolones
will need to be continually monitored in the changing therapeutic environment. Antibiotic drug
choice will remain difficult in the presence of increasing resistance, but introduction of the new
quinolones has created a new and exciting era in antimicrobial chemotherapy.
